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Abstract

Guava (Psidium guajava L.) is a highly valuable plant for ethnomedicine, which has been massively accepted and utilized in the regions of Asia, Africa and South America for the cure of diarrhea, diabetes, infections, inflammatory diseases, wounds, and metabolic disorders. The utilization of guava leaves is very effective given that their phytochemical composition is abundantly endowed with flavonoids (quercetin, kaempferol), phenolic acids, tannins, terpenes, alkaloids, essential oils, minerals, and vitamins, which, when used together, lead to potent antioxidant, antimicrobial, anti-inflammatory, antidiabetic, anticancer, and hair growth–promoting effects. The current paper is a review of the aspects of relative importance, phytochemical variability, pharmacological properties, analytical characterization, and the influence of genetic and environmental factors on phytochemical composition. The use of advanced analytical tools such as HPLC, LC-MS, GC-MS, UPLC-QTOF-MS, and NMR account for the precise identification and standardization of bioactive constituents supplemented by strong validation parameters compatible with ICH Q2(R1), AOAC, and WHO guidelines. The overall extraction effectiveness is modern green technology-wise made possible by the methods such as ultrasound-assisted, microwave-assisted, enzyme-assisted, and supercritical fluid extraction. Hence, the detailed phytopharmacological profile of guava leaves opens up possibilities for them to be a sustainable, biocompatible source of natural therapeutic agents for pharmaceutical, nutraceutical, and cosmeceutical applications.

Keywords

Guava leaves, Phytochemicals, Anti-inflammatory and antioxidant activities, Analytical characterization, Extraction techniques

Introduction

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Guava​‍​‌‍​‍‌​‍​‌‍​‍‌ (Psidium ‍‌‍‍‌‍‌‍‍‌Guajava L.) is a tropical evergreen shrub of the Myrtaceae family and is spread in a diverse range of regions in Asia, Africa, and South America. A highly nutritious, medicinal, and economically valuable plant, guava is not only recognized as a fruit crop but also as a major one of the bioactive compounds' sources (Dube et al., 2021; M. Kumar et al., 2021). Accordingly, guava has been a primary source of various healthcare treatments in the indigenous systems of medicine (Auyrveda, Unani, and different folk practices) such as diarrhea, diabetes, cough, inflammation, wounds, and infections (Das & Goswami, 2019; Shaheena et al., 2019). Guava parts, especially leaves, have been traditionally used for common ailments since its therapeutic properties are diverse and they are easily available (Altemimi et al., 2017; Sampath Kumar et al., 2021). Guava leaves are an ethnomedicinal resource that has been recognized by many cultures worldwide. In Indonesia, they are used for the treatment of diarrhea and gastroenteritis. Traditional uses are currently backed by pharmacological studies that reveal the same antioxidant, antibacterial, and anti-inflammatory effects that are to the phytochemical constituents of the ‍‌‍‍‌‍‌‍‍‌leaf  (Gutiérrez-Grijalva et al., 2018; Shaheena et al., 2019). P. guajava phytochemical‍‌‍‍‌‍‌‍‍‌survey reveals that it is a rich source of various kinds of metabolites such as flavonoids, tannins, terpenoids, alkaloids, and saponins. Being the major one, quercetin is very instrumental as a strong antioxidant and reduce the production of inflammatory mediators (Denny et al., 2013; Omcl0205_0270, n.d.).  The health-supporting antioxidant attributes of the polyphenolic constituents present in the leaves can greatly alleviate the oxidative problems linked with chronic illnesses of a nature like diabetes, cardiovascular diseases, and cancer (Mohapatra et al., 2024; Vaibhavi et al., 2024). The latest research results also reveal that the leaves have the potential to regulate androgen activity and stimulate hair growth (Madaan et al., 2018). Guava leaves are a renewable, biodegradable, and biocompatible source of multifunctional bioactives. The addition of guava leaf extracts to food coatings, personal-care products, and pharmaceutical preparations provides antimicrobial protection and aligns with the “green” and “clean-label” movement (Sanker et al., 2024; Thanh Phong et al., 2025).

1.1 History of Psidium​‍​‌‍​‍‌​‍​‌‍​‍‌ guajava

Psidium​‍​‌‍​‍‌​‍​‌‍​‍‌ guajava L.'s past can be traced back to the time before the Columbian era when the native people of Central and South America, mainly Peru and Mexico, first domesticated the plant. Archaeobotanical evidence indicates that guava was planted as long ago as 2500 BCE and was not only eaten but also used in healing and rituals. Its spread in the world to tropical and subtropical areas is due to Spanish and Portuguese navigators in the 16th century who took it to India, Southeast Asia, and Africa. Guava in India was termed the “poor man’s apple” as it was loaded with nutrients and cheap, and it got prominent place in Ayurvedic and Unani medicine to be the cure of digestive and metabolic disorders (Das & Goswami, 2019). Traditional healers administered guava leaves and bark extracts to heal diarrhea, dysentery, wounds, and inflammation (Shaheena et al., 2019). Guava, by 19-20 centuries, became a major horticultural and medicinal crop in Asia and Africa, with the scientific exploration revealing the bioactive compounds like flavonoids, tannins, and triterpenoids (Denny et al., 2013).

AIM AND OBJECTIVES

The primary objective is to provide a complete understanding of Psidium guajava L. leaf bioactives by integrating ethnomedicinal relevance, phytochemical composition, and pharmacological importance (Vaibhavi et al., 2024).

OBJECTIVES:

  1. To provide traditional uses and their scientific care.
  2. To determine phytochemical sections accountable for the physiological consequences.
  3. Pharmacological activities such as antioxidant, antimicrobial, anti-inflammatory, antidiabetic, anticancer, and hair growth-promoting properties.
  4. Promote the application of modern pharmaceutical, nutraceutical, and industry with the safety, sustainability, and future research possibilities.

 

1.3 Phytopharmacological Effects of Guava Leaves

Extensive​‍​‌‍​‍‌​‍​‌‍​‍‌ research on guava leaves reveals to us their various pharmacological and therapeutic attributes. Guava leaves become the source of their antioxidant power through flavonoids and phenols. These substances capture the radicals and recover the user's own defense. The anti-inflammatory features of guava leaves come from the impact of these natural constituents on the cyclooxygenase and lipoxygenase pathways. As the result, prostaglandin and leukotriene synthesis decreases. The antimicrobial capacity of guava leaves is the best illustration of the relationship between the bacterial membrane rupture and enzyme activity inhibition in bacteria like Staphylococcus aureus, Escherichia coli, and Candida albicans (Laily et al., 2015; Ruksiriwanich et al., 2022). Besides that, the herbal drug also delivers very strong antidiabetic effects by means of inhibition of α-glucosidase and α-amylase enzymes, which leads to a decrease in postprandial hyperglycemia. The herbal extracts have also been revealed to exhibit anticancer effects on breast, prostate, and liver cancer through apoptosis, cell proliferation, and signaling cascades changes mechanisms. Furthermore, guava leaf components are capable of immune system modulation, liver, and heart protection as well (Pawar et al., 2024; Sanker et al., 2024).

  1. Phytochemical Composition

Phytochemicals in guava leaves that make them highly effective for treatment. The primary groups are flavonoids, phenolic acids, tannins, terpenoids, alkaloids, proteins, essential oils, and essential minerals/vitamins.

Table 1. Composition of Psidium guajava Leaves in terms of ​‍​‌‍​‍‌​‍​‌‍​‍‌Phytochemicals.

Category

Key Compounds

Main Activities

Important Findings

References

Flavonoids

Quercetin, kaempferol, guaijaverin, rutin

Antioxidant, anti-inflammatory, antimicrobial

Major bioactives; levels 29.66–92.38 mg QE/g DW

(Díaz-de-Cerio et al., 2023; Xu et al., 2020)

 

Phenolic Compounds

p-Coumaric, caffeic, ferulic, sinapic acids

Antioxidant, antidiabetic, antimicrobial

Higher in leaves; confirmed by HPLC–MS/MS

(Ashraf et al., 2016; Chiari-Andréo et al., 2017; Jayachandran Nair et al., 2017)

Tannins

Hydrolyzable & condensed tannins

Antioxidant, antibacterial, enzyme inhibition

Condensed tannins ~17.79 mg TAE/g DW

(Chiari-Andréo et al., 2017; Farag et al., 2020; Konczak & Zhang, 2004)

Terpenes & Terpenoids

Caryophyllene, nerolidol, limonene; triterpenes (ursolic, oleanolic, betulinic acids)

Anti-inflammatory, anticancer, antidiabetic

Terpenoids ~71.65% of essential oil; 50 volatiles detected by GC–MS

(Arain et al., 2019; Ashraf et al., 2016; Lima et al., 2015)

Alkaloids

Pyrrolidine, piperidine, indole, quinoline derivatives

Antimicrobial, pharmacological activity

High content (219.06 mg/g DW); ethanol best solvent

(Chandran et al., 2020; George, 2021; Yumita et al., 2023)

 

Proteins

Essential amino acids

Nutritional, metabolic functions

~9.73% protein; good plant-based nutritional source

(Jassal & Kaushal, 2019; Zaminur Rahman et al., 2013)

Essential Oils

β-Caryophyllene, α-pinene, 1,8-cineole, limonene

Antioxidant, antimicrobial, anti-inflammatory

50–64 volatile compounds; sesquiterpenes dominant

(Lee et al., 2012; Soliman et al., 2016)

Minerals & Vitamins

Ca, K, Mg, Fe, Na, Mn, B, Vit C, Vit B

Bone health, immunity, metabolism

High mineral content; Vit C ~103 mg/100 g DW

(Adrian et al., 2015)

 

Guava​‍​‌‍​‍‌​‍​‌‍​‍‌ leaf is a rich source of flavonoids such as quercetin and kaempferol which are the main contributors of antioxidant, anti-inflammatory, and antimicrobial effects. Phenolic acids like caffeic and ferulic acids help in antioxidant and antidiabetic activity. Terpenes/terpenoids such as caryophyllene, nerolidol, and limonene are anti-inflammatory, anticancer, and metabolic-regulating agents, while triterpenes like ursolic and oleanolic acid exhibit potent antidiabetic and anticancer effects. Alkaloids are the source of additional antimicrobial activity. Besides these, essential oils, plant proteins, minerals, and vitamins further enhance the leaves’ nutritional and therapeutic ​‍​‌‍​‍‌​‍​‌‍​‍‌value.

  1. Analytical Characterization of Phytochemicals

Analytical​‍​‌‍​‍‌​‍​‌‍​‍‌ characterization is basically the initial move in figuring out the chemical makeup, therapeutic potential and the quality of P. guajava leaves. Compounds identification, quantification and validation are made possible by the use of advanced instruments such as HPLC, LC–MS, GC–MS, and UPLC–QTOF–MS. HPLC is the one that offers very accurate quantification, LC–MS and UPLC–QTOF–MS give more pieces of evidence for the structural and metabolomic profiles, while GC–MS is used for the identification of volatile components. NMR spectroscopy is there to provide further support during structural confirmation. Altogether, these methods make it possible to perform the complete chemical fingerprinting which is a very important factor in reproducibility and standardization of guava-derived pharmaceuticals and ​‍​‌‍​‍‌​‍​‌‍​​‍​‌‍​‍‌​‍​‌‍​‍‌nutraceuticals (Emam et al., 2025; Huynh et al., 2025a).

    1. Purpose of Analytical Characterization
    1. To uncover the main bioactive phytochemical components and their quantities in Psidium guajava leaves.
    2. To verify the structural features of the major secondary metabolites through various analytical platforms.
    3. To create repeatable methods that would ensure the presence of the same quality both in experimental and commercial samples.
    4. To set up a scientific base for the control of quality and standardization of the products made of guava.
    5. To secure therapeutic effectiveness and chemical consistency of bioactive compounds from guava by means of validated methods.
    6. To provide a basis for metabolomics studies that explore biochemical pathways and compound interactions in guava leaf matrices (Emam et al., 2025).

3.2 Analytical Methods

3.2.1 High-Performance Liquid Chromatography (HPLC)

HPLC is the most common method to determine the amount of phenolic and flavonoid compounds in guava leaves. To detect the compounds, UV or DAD detectors are used which are based on the compounds' polarity and retention time. HPLC–MS/MS is used to quantify the major phenolics such as gallic acid, ellagic acid, catechin, quercetin, and kaempferol. The technique is quite precise, speedy, and is in good terms with the routine quality control process(Huynh et al., 2025a).

3.2.2 Liquid Chromatography–Mass Spectrometry (LC–MS / LC–ESI–MS/MS)

LC–MS chromatographic separation with the molecular detection capability of mass spectrometry. This makes it possible to accurately identify the molecular structure of semi-polar compounds such as flavonoid glycosides, alkaloids, triterpenoids, and phenolic esters. ESI facilitates the detection in both positive and negative ion modes that are compatible with complex phytochemical mixtures. (Costa De Camargo et al., 2025; El Sayed et al., 2020).

3.2.3 Gas Chromatography–Mass Spectrometry (GC–MS)

GC–MS is a technique that can be used to identify the volatile and low molecular weight compounds. Some of the components that P. guajava has and that GC-MS can detect are β-caryophyllene, 1,8-cineole, limonene, palmitic acid, and linoleic acid. Also, the comparison with NIST and Wiley libraries facilitates accurate confirmation of compounds (El Sayed et al., 2020; Huynh et al., 2025a).

3.2.4 Ultra-Performance Liquid Chromatography–Quadrupole Time-of-Flight–Mass Spectrometry (UPLC–QTOF–MS)

By combining UPLC-QTOF fast separation with high-resolution mass detection, it allows for metabolomics at the trace level. Besides, it can easily detect the minor phenolic derivatives and flavonoid glycosides besides giving the most preferable chemical fingerprint for the standardization process (Emam et al., 2025).

3.2.5 Nuclear Magnetic Resonance (NMR) Spectroscopy

NMR offers a non-destructive and highly detailed approach to the structural elucidation of both primary and secondary metabolites. With the help of NMR, the data obtained from LC–MS and GC–MS can be supported through the confirmation of the structural features of flavonoids, terpenoids, and phenolic acids (Emam et al., 2025).

Table 2. Major Analytical Methods for Characterization of Guava Leaf Phytochemicals

Chromatographic and spectroscopic instruments provide a thorough metabolomic profile of the leaves of Psidium guajava. HPLC is the one that measures phenolics, LC–MS/UPLC–QTOF–MS identify metabolites, GC–MS identifies volatiles and NMR confirms structures. They facilitate reliable standardization as well as bioactivity correlation when working ​‍​‌‍​‍‌​‍​‌‍​‍‌together.

3.2 Validation Parameters

Validation​‍​‌‍​‍‌​‍​‌‍​‍‌ of analytical methods is essentially setting the stage for the data obtained to be considered fair, trustworthy, and repeatable. As per ICH Q2(R1), AOAC, WHO, a process that stipulates the use of analytical methods to achieve their intended goals. Guava leaves which are made up of complex compounds and where co-elution of the matrix is very likely, validation determines the scientific robustness of each method thus it is the main point that data can be trusted for research, regulatory submission, and industrial usage (Emam et al., 2025; Huynh et al., 2025a).

Method Validation Purposes

    1. To emphasizing the analytical procedures accuracy, precision, and repeatability.
    2. To ensuring the trace detection of low-abundance metabolites through LOD and LOQ that are well-defined.
    3. The efficiency of the plant matrix's extraction and recovery is to be validated.
    4. Instrumental reproducibility is to be assured and inter-laboratory variations eliminated.
    5. To standardize analytical workflows for quality control and formulation development based on ​‍​‌‍​‍‌​‍​‌‍​‍‌guava.

3.3.1. Validation​‍​‌‍​‍‌​‍​‌‍​‍‌ Parameters and Their Basis

Validation undertaken in compliance with worldwide standards (ICH Q2(R1), AOAC, WHO) serves to check if the new analytical routine can stand up to the challenge posed by its intended purpose. The plant extracts being highly complex and overlapping in phytochemical content. The validation not only supports the scientific robustness but also elevates the data quality for use in research, regulatory approval, and industrial application arenas (Emam et al., 2025; Huynh et al., 2025a).

Phytochemical validation of Psidium guajava extracts is the crucial to finding reliable analytical results. The key parameters are accuracy, precision, linearity, sensitivity (LOD/LOQ), recovery, robustness, reproducibility, and selectivity are the factors that confirm the methods such as HPLC, LC–MS, GC–MS, and UPLC–QTOF–MS are capable of generating reliable data.

3.4​‍​‌‍​‍‌​‍​‌‍​‍‌ Interpretation and Significance

1. Analytical profiling of Psidium guajava leaves confirms reliable, reproducible, and authentic phytochemical data.

2. Advanced tools (HPLC, LC–MS, UPLC–QTOF–MS, GC–MS, NMR) offer a complete chemical of major and minor bioactives.

3. Validation parameters such as accuracy, precision, linearity, robustness, reproducibility meets ICH Q2(R1), AOAC, WHO standards (Emam et al., 2025).

4. Higher phenolic/flavonoid content (HPLC, LC–MS) relates with antioxidant and anti-inflammatory effects.

5. Terpenes identified by GC–MS contribute to antimicrobial and antidiabetic activities.

6. Validated methods confirm quality assurance for guava extracts.

7. They provision the development of evidence-based, standardized herbal formulations.

8. Empower extensive applications in pharmaceutical, nutraceutical, and cosmeceutical industries.

4.​‍​‌‍​‍‌​‍​‌‍​‍‌ Factors Affecting Phytochemical Yield and Composition

The qualitative and quantitative phytochemical aspects of biologically active substances in Psidium guajava leaf are affected by numerous genetic, environmental, and methodological factors. These factors is key to phytochemical recovery optimization and extract quality consistency (Huynh et al., 2025a; Imtara et al., 2025; A. Kumar et al., 2023; Mugao, 2024; Rawat et al., 2025).

    1. Genetic Variation and Cultivar Differences
  • The main factors determining the secondary metabolite profile is the selection of different guava cultivars.
  • The cultivars abundant in antioxidants and essential oils are those that most probably show increased biosynthetic gene activity.

4.2 Environmental Conditions

  • The nutrients of the soil are the core regulators of enzyme activities that are related to the making of phenolic compounds.
  • Temperature, rainfall, sunlight, and humidity have an effects on the levels of flavonoids, tannins, and essential oils.

4.3 Harvesting Stage

  • The new leaf parts will have higher vitamin C, flavonoids, and antioxidant contents.
  • The mature leaves will be higher in tannins and will contain more chemically stable polyphenols. It is the proper harvesting stage that decides the therapeutic value of the product.
    1. Drying and Storage Methods
  • Both freeze drying and air drying can better maintain heat-sensitive compounds as compared to oven or sun drying.
  • The best storage of the product will be in a dark airtight container with a low level of moisture to prevent oxidation.

4.5 Solvent Polarity and Extraction Time

  • Polar solvents (ethanol, methanol, water): Extract flavonoids and phenolics.
  • Non-polar solvents (hexane, chloroform): Extract terpenes and fatty acids. Extraction time necessity be enhanced to avoid deprivation while ensuring full compound recovery.

4.6 pH and Temperature of Extraction Medium

  • The solubility of phenolics is improved when the medium is slightly acidic, while saponins are better extracted from an alkaline medium.
  • The best temperatures for extraction are 40–60°C because in this range the compounds diffuse from the matrix but they are not degraded.

5. Extraction Technologies

5.1 Conventional Extraction Methods

Conventional extraction methods refer to the traditional procedures, which have been used extensively to obtain bioactive compounds from plant-based materials. These methods mainly depend on solvent diffusion and solubility deviations of phytochemicals in plant tissues (Food Process Engineering and Technology Second Edition, n.d.). The main characteristic of extraction methods are maceration, percolation, and Soxhlet extraction.

      1. Maceration

Maceration​‍​‌‍​‍‌​‍​‌‍​‍‌ is a straightforward technique that includes soaking a powdered plant in solvents (ethanol, methanol, ethyl acetate) at room temperature for 24-72 hours. The compounds are removed by diffusion. This method is suitable for thermolabile molecules (Bouchoukh et al., 2019). This method is simple and cheap but it is slow and produces lower yields than the advanced extractions, with the yields of 4.5% (chloroform) and 8.2% (ethyl acetate) being reported (Díaz-de-Cerio & Trigueros, 2025). Maceration is still a method of choice for many due to its ease, safety, and low operational cost (Bouchoukh et al., 2019).

      1. Percolation

Percolation is a variant of maceration that enables the continuous flow of the solvent through the plant material, thus improving mass transfer and extraction efficiency. In this process, the solvent is allowed to pass through a column or container full of plant material at a flow rate which is under control (Food Process Engineering and Technology Second Edition, n.d.). This method can also be used in large-scale production due to its reproducibility and the fact that solvent utilization is more efficient.

      1. Soxhlet extraction

Soxhlet extraction is a continuous hot extraction process where the solvent is successively evaporated and condensed to remove the soluble compounds from the plant materials (Bai et al., 2015). The system enables fresh solvent to be continuously used to wash the sample, thereby ensuring complete extraction. Heat improves solubility and diffusion, thus Soxhlet method is especially good for the extraction of heat-stable compounds. Extraction times are usually between 6 and 48 hours depending on the solvent and the plant matrix (Bai et al., 2015). Even though Soxhlet extraction produces higher quantities of bioactive compounds than maceration or decoction (Ayembilla et al., 2023). Conventional extraction methods, which are the basis of phytochemical studies, are gradually being substituted or supported by advanced techniques that are characterized by higher yield, selectivity, and efficiency ​‍​‌‍​‍‌​‍​‌‍​‍‌(Bhagya Raj & Dash, 2020; Sampath Kumar et al., 2021).

5.2 Modern Extraction Methods

5.2.1​‍​‌‍​‍‌​‍​‌‍​‍‌ Ultrasound-Assisted Extraction (UAE)

Ultrasound-Assisted Extraction (UAE) is a green, quick, and operative method of procurement of bioactive compounds from plant materials (Carreira-Casais et al., 2021). The method includes the use of ultrasonic waves (20–100 kHz) that produce cavitation bubbles in the solvent (Fu et al., 2020).

Major effects of ultrasound

  1. Thermal effect: The thermal effect supports solubility and diffusion of compounds (Qiu et al., 2020).
  2. Mechanical effect: The mechanical effect energizes the solvent to penetrate the particle by vibrating it (Wen et al., 2018).
  3. Cavitation effect: The microjets (200–700 m/s), high temperature (≈5000 K), and pressure (≈2000 atm) produced as a result of cavitation effect help extraction to be more efficient (Shen et al., 2023).

Compared to conventional methods, UAE offers shorter extraction time, less solvent consumption, and higher yield (Chemat et al., 2017). The method is mostly safe for heat-sensitive and polar phytochemicals (Zhang et al., 2021). The UAE is determined by factors such as ultrasonic power, temperature, solvent polarity, extraction time, and solid-to-solvent ratio which must be optimized carefully (Kong et al., 2015; Vajira Bulugahapitiya et al., 2024).

 5.2.2​‍​‌‍​‍‌​‍​‌‍​‍‌ Microwave-Assisted Extraction (MAE)

Microwave-Assisted Extraction (MAE) is a fast, energy-efficient method that employs non-ionizing electromagnetic waves (300 MHz–300 GHz) to separate bioactive compounds from plants. The microwaves heat the material through ionic conduction and dipole rotation, which breaks the cell walls, increases porosity, and releases the intracellular compounds, thus intensifying the mass transfer and the yield (Szliszka et al., 2009). The performance of MAE is dictated by the dielectric characteristics of the solvent and plant material (Gil-Martín et al., 2022). To attain an optimum balance between the yield and stability of the compounds (Frosi et al., 2021; Gupta et al., 2024; Vlachoudi et al., 2023).  MAE yields are very high, in comparison with less solvent is required and energy consumption is low, while the time of extraction is significantly shortened when compared with conventional methods (Valisakkagari et al., 2024a). Phenolics and pectins extraction from the fruit by-products such as pomelo, tangerine, pineapple, and banana peels have been the subject of research works applying MAE (Benmebarek et al., 2024; García-Martín et al., 2023). It demonstrated a green score (GS) of 0.49 at the point of 1.8 min extraction, thus indicating low energy consumption and high efficiency(Mali & Kumar, 2023).

5.2.3 Enzyme-Assisted​‍​‌‍​‍‌​‍​‌‍​‍‌ Extraction

Enzyme-Assisted Extraction (EAE) is a green, and non-thermal procedure that involves using specific enzymes to dismantle plant cell walls and, in this way, set free bioactive compounds in a very short time (Boateng & Clark, 2024). The cellular walls are hydrolyzed by the enzymes cellulases, hemicellulases, pectinases, and proteases, and the transmission of mass along with permeability is enlarged (Barbosa et al., 2021; Łubek-Nguyen et al., 2022). EAE hinges on features such as enzyme type, concentration, temperature, pH, extraction time, and particle size. Conditions that are gentle (≈40 °C, optimal pH) facilitate enzyme activity and the production of thermolabile compounds is still possible (Fatima et al., 2024; Valisakkagari et al., 2024a). EAE can boast of great features such as the use of green solvents (water/buffers), low energy consumption, high selectivity, and the integrity of the compounds being preserved. It is performed in a simple apparatus and is a way of producing phenolics, flavonoids, lipids, proteins, and pectins from different plant wastes. The principles of green chemistry, EAE is very mild and sustainable and, therefore, does not produce much waste and has a low impact on the environment (Gómez-García et al., 2012).

5.2.4 SFE (Supercritical Fluid Extraction)

Supercritical Fluid Extraction (SFE) is an innovative extraction technique that requires a solvent to be in its supercritical state which means that the temperature and pressure have to be beyond the critical point (Tc and Pc) (Casquete et al., 2022). The extraction method is based on the principle of diffusion of solutes from the solid matrix into the extraction medium (Díaz-de-Cerio & Trigueros, 2025).

Parameters of SFE

The effectiveness of SFE is controlled by various factors - The pressure, the temperature, the flow rate, the extraction duration, the particle size and the use of co-solvent.

  1. Pressure: Up to 30 MPa rises CO₂ density and yield, higher levels raise cost/energy (Casquete et al., 2022).
  2. Temperature: Optimal 35–60 °C to avoid deprivation, higher temp increases vapor pressure but lowers CO₂ density (Romano et al., 2022).
  3. Co-solvent: The accumulation of a few drops of ethanol or methanol make simpler the extraction of phenolics and flavonoids.
  4. Flow rate & time: Advanced stream and extended time increase mass transfer; smaller particles expand diffusion.

SFE​‍​‌‍​‍‌​‍​‌‍​‍‌ has many features that make it superior to traditional solvent extraction (Díaz-de-Cerio & Trigueros, 2025). SFE is a green technology in line with green chemistry principles through the use of non-toxic CO₂, the near elimination of solvent waste, and the production of quality bioactives (Díaz-de-Cerio & Trigueros, 2025; Romano et al., 2021, 2022).

Table: Extraction Technologies

Technologies

Method

Principle & Mechanism

Advantages

Disadvantages

Yield Data

Conventional

Maceration

Soaking plant material in solvent at room temp for diffusion-based extraction.

Simple, inexpensive, safe for thermolabile compounds.

Time-consuming, low yield.

Guava leaf: 4.5–8.2% yield (chloroform–ethyl acetate).

 

Percolation

Continuous solvent flow through plant bed enhances mass transfer.

Higher efficiency, reproducible, scalable.

More equipment and solvent use.

Widely used for industrial extracts.

 

Soxhlet Extraction

Continuous hot extraction via repeated evaporation-condensation cycles.

Complete extraction, higher yield, efficient solvent use.

Long time, high energy, not eco-friendly.

Psidium guajava: 1.8–8.07% yield (methanol best).

Modern / Green

Ultrasound-Assisted Extraction (UAE)

Cavitation bubbles disrupt cell walls, improving diffusion.

Short time, low solvent, high yield, eco-friendly.

High power may degrade compounds.

Psidium guajava polysaccharides: 9.2% yield.

 

Microwave-Assisted Extraction (MAE)

Microwaves heat solvent and matrix through dipole rotation and ionic conduction.

Very fast, energy-efficient, high yield, scalable.

Risk of overheating/degradation.

Green score (GS): 0.49 (efficient).

 

Enzyme-Assisted Extraction (EAE)

Enzymes degrade cell wall polymers, freeing bioactives.

Mild, selective, non-thermal, preserves bioactivity.

Enzymes costly, may deactivate.

GS = 0.1–0.54; high selectivity and yield.

 

Supercritical Fluid Extraction (SFE)

CO₂ at supercritical conditions dissolves and extracts solutes efficiently.

Solvent-free, pure extracts, eco-friendly, selective.

Expensive equipment, high pressure.

GS = 0.49 ± 0.09; moderately green.

Extraction​‍​‌‍​‍‌​‍​‌‍​‍‌ technologies have different stages in depuration of bioactive compounds. They go from very slow and solvent-consuming traditional methods to very fast and solvent-free techniques. Modern methods such as UAE, MAE, EAE and SFE allow obtaining higher yields, selectivities and efficiencies in less time and with less solvent.

6. Synergistic and Molecular Insights

6.1 Synergistic​‍​‌‍​‍‌​‍​‌‍​‍‌ Effects Among Bioactives

  • Flavonoids, tannins, and polyphenols present in guava leaves exhibit synergistic interactions that enhance overall biological activity.
  • The combined action of these bioactive compounds results in stronger antioxidant and anti-inflammatory effects compared to individual constituents.
  • Synergistic mechanisms contribute to improved reactive oxygen species (ROS) scavenging through multiple molecular pathways. The interaction of different phytochemicals enhances antimicrobial efficacy by targeting multiple biological sites simultaneously (Huynh et al., 2025b).

6.2 Molecular docking studies

Computational molecular docking is a structure-based approach used to predict the preferred orientation of a ligand within the binding site of a target protein. Docking simulations evaluate ligand–protein interactions using scoring functions that estimate binding affinity and complex stability. These studies help in identifying potential inhibitors by analyzing interaction strength, binding pose, and energetic favorability, thereby supporting drug discovery and lead optimization processes (Bhagat et al., 2021; Saber et al., 2021).

6.3 Mechanistic pathways and enzyme target interactions

Guava bioactives primarily intervene antioxidant and anti-inflammatory processes by directly targeting enzymes and cellular signaling molecules. These action routes eventually lead to the alleviation of oxidative stress and the reduction of inflammatory mediator ​‍​‌‍​‍‌​‍​‌‍​‍‌release (Huynh et al., 2025b).

  • Integrated Mechanistic Outcomes: Guava bioactives are capable of removing oxidative stress as well as inflammation concurrently through the process of ROS scavenging, antioxidant enzymes activation, and COX-2, iNOS, and cytokines inhibition.

Thus, these actions, which interplay, result in skin and tissue protection, prevention of cellular damage, and the induction of inflammatory conditions healing ​‍​‌‍​‍‌​‍​‌‍​‍‌acceleration (Huynh et al., 2025b).

7. Recent Trends and Innovations (2023–2025)

7.1 Nanotechnology integration

  • Nanotechnology plays an important role in modern pharmaceutical research by enabling the design and development of nanoscale drug delivery systems.
  • The integration of nanotechnology improves drug solubility, stability, and bioavailability while allowing targeted and controlled drug release.
  • Nanocarriers such as nanoparticles enhance therapeutic efficiency by improving interaction with biological systems and reducing unwanted side effects. Thus, nanotechnology-based approaches contribute significantly to the advancement of drug delivery and treatment strategies (Albadawi et al., 2024).
    1. AI-driven formulation and process modelling
  • Artificial intelligence techniques such as machine learning and data-driven models are used to optimize formulation design by analyzing complex formulation variables.
  • AI-based process modelling helps predict critical process parameters, improving consistency, efficiency, and product quality.
  • Predictive algorithms reduce trial-and-error experimentation, saving time, cost, and material during formulation development.
  • Integration of AI supports process control and decision-making by enabling accurate simulation and optimization of manufacturing workflows (Dirgule et al., 2025).

7.3 Green extraction and eco-friendly formulation design

  • Green extraction approaches focus on the use of environmentally safe solvents and sustainable processing techniques to obtain bioactive compounds while minimizing energy consumption and chemical waste.
  • These methods aim to reduce environmental impact and improve extraction efficiency without compromising product quality.
  • Eco-friendly formulation design further emphasizes the use of biodegradable materials and safer excipients to enhance stability and effectiveness while maintaining sustainability. Such strategies support the development of environmentally responsible pharmaceutical products (Imtara et al., 2025).

7.4 Advances in cosmeceutical and pharmaceutical applications

  • Bioactive phytochemicals obtained through green extraction methods are increasingly used in cosmeceuticals for their antioxidant, anti-inflammatory, and anti-aging benefits.
  • Natural compounds such as polyphenols and flavonoids help protect the skin from UV-induced oxidative stress and cellular damage, offering safer alternatives to synthetic ingredients.
  • In pharmaceutical formulations, plant-derived bioactives demonstrate potential in antimicrobial, anti-inflammatory, wound-healing, and anticancer applications.
  • Green-extracted phytochemicals show enhanced stability and bioavailability, while eco-friendly extraction processes support sustainable and regulatory-compliant product development (Valisakkagari et al., 2024b).

8. Challenges and Future Perspectives

8.1 Standardization and clinical validation

 A major challenge in guava-based formulations is variability in phytochemical composition due to differences in source, processing, and extraction methods. Although standardization parameters for simplicia and extracts have been established, their consistent application remains limited. In addition, the lack of sufficient clinical validation restricts therapeutic translation. Future efforts should focus on harmonized standardization protocols and well-designed clinical studies to ensure safety, efficacy, and regulatory acceptance (Suswidiantoro et al., n.d.).

8.2 Bioavailability and stability issues

The guava leaf bioactive, e.g. the flavonoids and polyphenols, are insoluble, have low penetration through the skin, and are readily degraded by atmospheric factors, therefore its therapeutic value in ointments is highly restricted. Nanotechnology-based delivery platforms such as nano emulsions, liposomes and polymeric nanoparticles can enhance solubility and sustained release to improve skin absorption (Khare et al., 2024).

8.3 Regulatory limitations

A significant hurdle in guava crop regulation is the lack of harmonized global and local standards, which complicates international trade and quality consistency. While conventional methods are well-established, the integration of modern techniques like genetic engineering faces strict regulatory and ethical scrutiny, limiting their widespread therapeutic and commercial acceptance. Additionally, mandatory adherence to environmental laws regarding pesticide use, water quality, and waste management remains a complex challenge for farmers. Future progress depends on creating unified standardization protocols and supportive legal frameworks to ensure safety, sustainability, and market competitiveness (Yadav et al., 2023).

9. Future Research and Directions

Research on the subject ought to primarily be done on large and well-controlled clinical trials that would substantiate the safety, dosage and efficacy of guava ointments. The predictions of bioavailability, stability, and release profiles can be improved with the assistance of AI, which can help in formulation.

9.1 Large-Scale Clinical Studies and Dosage Optimization

The future studies must mostly involve large, controlled, clinical trials that will establish the safety, dosage and efficacy of guava ointments. Bioavailability, stability as well as release behavior can be better predicted using AI-driven formulation tools. These will have the potential to accelerate the creation of the optimized nano-ointments significantly (Bouchoukh et al., 2019; Łubek-Nguyen et al., 2022).

9.2 Advanced Formulation Research with AI Integration

The AI and machine learning tools can significantly simplify the research on the formation of the guava ointment as it will be able to simulate the interactions of the scientific elements and to predict the stability, permeability, and release kinetics (Dirgule et al., 2025).

    1. Multi-Herbal Synergistic and Personalized Medicine

Synergistic action of complementary herbal constituents can have a great impact in enhancing the therapeutic effects of the guava leaf extracts. Pytochemicals interactions can be predicted with the help of molecular docking. In vitro studies can confirm the presence of synergistic interactions. Multi-herbal formulation efficacy can become a guide in in vivo studies (Huynh et al., 2025b).

    1. Sustainable, Green Manufacturing and Extraction Protocols

The extracting green methods are ultrasound-, microwave-, supercritical fluid-, and enzyme- assisted. Their production is still in a phase as they require to be refined further to enhance the purification and the yield of phytochemicals of guava. The project is being undertaken to ensure that the minimal effects of production on the environment are realized (Valisakkagari et al., 2024b).

    1. Novel Delivery Systems Targeting Specific Skin Layers

The steps to take next should involve the potential more advanced delivery methodologies like nanoplarticles with stimuli-sensitive abilities, microneedle patches, transdermal systems as well as bioadhesive polymers that have the capabilities to allow penetration or retention of guava bioactives in specific parts of the skin(Chiari-Andréo et al., 2017; Valisakkagari et al., 2024b).

CONCLUSION

Guava​‍​‌‍​‍‌​‍​‌‍​‍‌ (Psidium guajava L.) leaves can be seen as a significant ethnomedicical and phytopharmacological source, being a potential attractive therapeutic agent. The​‍​‌‍​‍‌​‍​‌‍​‍‌ first thing to come to mind as their bioactive substances are the flavonoids, the phenolic acids, the tannins, the terpenoids, the alkaloids, the essential oils, the minerals, and the vitamins, which are the major contributors to the pharmacological versatility because the activities mentioned cover a wide range of antioxidant, antimicrobial, anti-inflammatory, antidiabetic, anticancer, hepatoprotective, cardioprotective, and hair growth–promoting. The chemical analysis and the quality standardization of the guava-derived products are very much facilitated by the application of advanced instrumental techniques such as HPLC, LC–MS, GC–MS, UPLC–QTOF–MS, and ​‍​‌‍​‍‌​‍​‌‍​‍‌NMR. Phytochemical production is largely determined by genetics, environment, and methodology parameters, thus there is a necessity for the standardization of harvesting, drying, and extraction stages. Present-day extraction methods—UAE, MAE, EAE, and SFE—are not only more productive and environmentally friendly than the traditional ones but also make it possible to achieve better yields with proper preservation of heat-sensitive substances. Guava leaves, in general, are a renewable, naturally decomposable, multifunctional material of nature-derived bioactives with major consequences for the contemporary pharmaceutical, nutraceutical, cosmeceutical, and food sectors. The ongoing research on metabolomics, formulation, standardization, and clinical validation will, in fact, facilitate their move from historically folk medicine to scientifically proven modern applications.

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Jannatul Firdaus
Corresponding author

Sharda University Greater Noida, Uttar Pradesh 201310, India

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Khushi Rastogi
Co-author

Sharda University Greater Noida, Uttar Pradesh 201310, India

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Anshika Yadav
Co-author

Sharda University Greater Noida, Uttar Pradesh 201310, India

Photo
Tanlaka Nuradin Fonyuy
Co-author

Sharda University Greater Noida, Uttar Pradesh 201310, India

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Shahnawaz Ahmad
Co-author

Jamia Millia Islamia, University, New Delhi-110025, India

Jannatul Firdaus*, Khushi Rastogi, Anshika Yadav, Tanlaka Nuradin Fonyuy, Shahnawaz Ahmad, Guava (Psidium guajava L.) Leaf Bioactives: From Phytochemical Characterization to Therapeutic and Technological Applications, Int. J. Med. Pharm. Sci., 2026, 2 (5), 310-328. https://doi.org/10.5281/zenodo.20073557

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