Fabrication, organoleptic evaluation and in vitro characterization of cream loaded with Carica papaya seed extract.

OBJECTIVE: The current study aimed to provide preliminary insights into potential biopharmaceutical applications of Carica papaya seed extract by evaluating its phytochemical and biological profiles. Furthermore, the study aimed to develop a stable oil-in-water (O/W) emulsion for the effective delivery of antioxidant-rich biologicals for cosmetic purposes. METHODS: The hydroethanolic (ethanol 80%: 20% water) extract of C. papaya seeds was prepared via maceration technique. The chemical composition was carried out through preliminary phytochemical screening and estimation of total phenolic contents (TPC) and total flavonoid contents (TFC). The biological profile of the extract was explored using various in-vitro antioxidant methods. The homogenization procedure was used to create a cream of O/W and various tests were applied to assess the stability of the emulsion. By keeping the emulsion at different storage conditions (8 ± 0.5°C, 25 ± 0.5°C, 40 ± 0.5°C, and 40 ± 0.5°C ± 75% relative humidity [RH]) for a period of 28 days), the physical stability parameters of the emulsion, including pH, viscosity, centrifugation, phase separation, and conductivity, as well as rheological parameters and organoleptic parameters (odor, color, liquefaction, and creaming), were assessed. RESULTS: The preliminary phytochemical screening assay revealed the presence of various plant secondary metabolites including alkaloids, phenolics, flavonoids, tannins, saponins, and quinones. The extract was found to be rich in TPC and TFC. The in vitro antioxidant study gave maximum activity in the DPPH method. The plant extract containing cosmetic cream exhibited remarkable stability during the entire research. Data gathered indicated that no phase separation or liquefaction was seen after the experimental period. Throughout the experimental period, a small variation in the pH and conductivity values of the base and formulation was seen. CONCLUSION: The findings suggest that the seed extract of C. papaya is a rich source of polyphenols with antioxidant potential and can be a promising alternative for the treatment of various ailments. The stability of emulsion paves the way for its utilization as a carrier for the delivery of 3% C. papaya seed extract and applications in cosmetics products.

Chemical Profiling, Formulation Development, In Vitro Evaluation and Molecular Docking of Piper nigrum Seeds Extract Loaded Emulgel for Anti-Aging.

Emulgel is a new innovatory technique for drug development permitting controlled release of active ingredients for topical administration. We report a stable emulgel of 4% Piper nigrum extract (PNE) prepared using 80% ethanol. The PNE-loaded formulation had an antioxidant activity of 84% and tyrosinase inhibition was 82%. Prepared formulation rendered spherical-shaped globules with high zeta potential (-45.5 mV) indicative of a stable system. Total phenolic contents were 58.01 mg GAE/g of dry extract whereas total flavonoid content was 52.63 mg QE/g of dry extract. Sun protection factor for PNE-loaded emulgel was 7.512 and formulation was stable without any evidence of physical and chemical changes following 90 days of storage. Gas chromatography-mass spectroscopy (GC-MS) revealed seventeen bioactive compounds in the PNE including monoterpenoids, triterpenoids, a tertiary alcohol, fatty acid esters, and phytosterols. In silico studies of GC-MS identified compounds show higher binding affinity in comparison to standard kojic acid indicating tyrosinase inhibition. It can be concluded that PNE-loaded emulgel had prominent antioxidant and tyrosinase inhibition and can be utilized as a promising topical system for anti-aging skin formulation.

Nanostructured Ethosomal Gel Loaded with Arctostaphylosuva-Ursi Extract; In-Vitro/In-Vivo Evaluation as a Cosmeceutical Product for Skin Rejuvenation.

BACKGROUND: Arctostaphylosuva-ursi(AUU) being rich in polyphenols and arbutin is known to have promising biological activities and can be a potential candidate as a cosmaceutical. Ethosomes encourage the formation of lamellar-shaped vesicles with improved solubility and entrapment of many drugs including plant extracts. OBJECTIVE: The objective of this work was to develop an optimized nanostructured ethosomal gel formulation loaded with AUU extract and evaluated for skin rejuvenation and depigmentation. METHODS: AUU extract was tested for phenolic and flavonoid content, radical scavenging potential, reducing power activity, and in-vitro SPF (sun protection factor) estimation. AUU loaded 12 formulations were prepared and characterized by SEM (Scanning Electron Microscopy), vesicular size, zeta potential, and Entrapment Efficiency (%EE). The optimized formulation was subjected to noninvasive in-vivo investigations after incorporating it into the gel system and ensuring its stability and skin permeation. RESULTS: Ethosomal vesicles were spherical in shape and Zeta size, zeta potential, PDI (Polydispersity Index), percentages of EE and in-vitro skin permeation of optimized formulation (F3) were found to be 114.7nm, -18.9mV, 0.492, 97.51±0.023%, and 79.88±0.013% respectively. AUU loaded ethosomal gel formulation was stable physicochemically and exhibited non-Newtonian behavior rheologically. Moreover, it significantly reduced skin erythema, melanin as well as sebum level and improved skin hydration and elasticity. CONCLUSION: A stable AUU based ethosomal gel formulation could be a better vehicle for phytoextracts than conventional formulations for cosmeceutical applications such as for skin rejuvenation and depigmentation.

Development of topical drug delivery system with Sphaeranthus indicus flower extract and its investigation on skin as a cosmeceutical product.

BACKGROUND: Cosmetics are the products used to beautify the skin. Emulsion is a fine dispersion of two or more immiscible liquids. Sphaeranthus indicus is claimed to be used for skin beautification in folk medicine. Multiple emulsion was formulated containing the extract of S indicus flowers. AIMS: This research study indicates that extract of S indicus flowers contains sufficient amount of polyphenols and also possess good antioxidant activity with mushroom tyrosinase inhibition activity. METHOD: Further, stable multiple emulsion was developed and stability testing was performed for 180 days by keeping the multiple emulsion at 8°C ± 1, 25°C ± 1, 40°C ± 1, and 40°C ± 1 with 75% ± 1 RH. Parameters checked were color change, phase distribution, viscosity, droplet size and size distribution, pH determination, and electrical conductivity. Sun protection factor (SPF) was determined which also showed promising results. Skin testing on human volunteers was done for 3 months after biosafety profiling of the most stable multiple emulsion. RESULTS: This also showed remarkable effects. Skin erythema, melanin, and sebum were reduced. Skin hydration and elasticity were increased. There was also reduction in the number of skin large and small skin pores. Skin spot area was also reduced by the use of multiple emulsion loaded with S indicus flower extract. ANOVA test showed that all the effects produced on skin were significant, ie, P ≤ .05. CONCLUSION: A stable multiple emulsion was developed which produced significant cosmetic effects on human skin.

Polymeric emulgel carrying Cinnamomum tamala extract: promising delivery system for potential topical applications

Currently, the use of natural compounds obtained from plants tremendously increased due to their promising therapeutic properties. The aim of this study was to formulate a stable emulgel formulation loaded with Cinnamomum tamala (CT) extract. The antioxidant activity of plant extract was determined by DPPH inhibition assay. The extract was successfully loaded into an emulgels using different concentrations of carbopol-940, liquid paraffin, emulsifying agents and preservatives. Preliminary stability study was performed of 17 CT emulgel formulations at accelerated temperature of 50 °C for 2-months. Organoleptic evaluation, centrifugation, globule size, pH, electrical conductivity and rheological studies were performed for a period of 90-days at different temperature including 8, 25, 40 and 40 °C ±75% RH. The CT extract showed promising antioxidant activity of about 81%. On the other hand, the CT loaded emulgel formulation displayed high physical stability at all tested conditions of temperature and time. However, slight decrease in pH and minimum increase in conductivity was observed at 40 and 40 °C±75% RH. The rheological examination of CT emulgel indicated the flow index values of all the samples kept at different temperatures were less than 1, demonstrated non-newtonian and pseudo-plastic nature of CT emulgel. Taken together, the CT emulgel formulation has been evinced to be an excellent addition in the field of topical formulations.

Transdermal patches: Design and current approaches to painless drug delivery.

Use of transdermal patches can evade many issues associated with oral drug delivery, such as first-pass hepatic metabolism, enzymatic digestion attack, drug hydrolysis and degradation in acidic media, drug fluctuations, and gastrointestinal irritation. This article reviews various transdermal patches available in the market, types, structural components, polymer role, and the required assessment tools. Although transdermal patches have medical applications for smoking cessation, pain relief, osteoporosis, contraception, motion sickness, angina pectoris, and cardiac disorders, advances in formulation development are ongoing to make transdermal patches capable of delivering more challenging drugs. Transdermal patches can be tailored and developed according to the physicochemical properties of active and inactive components, and applicability for long-term use. Therefore, a number of chemical approaches and physical techniques for transdermal patch development are under investigation.

Phytocosmeceutical formulation development, characterization and its in-vivo investigations.

Several plants found rich in flavonoid, polyphenols, and antioxidants reported antiaging, oppose inflammation and carcinogenic properties but have rarely been applied in dermatology. The present study was an active attempt to formulate a stable phytocosmetic emulsion system loaded with 2% pre-concentrated Prosopis cineraria bark extract, aiming to revive facial skin properties. In order to obtain potent therapeutic activities, we first prepared extracts of stem, leaves, and bark and screen them on basis of phenolic, flavonoids contents and antioxidant, antibacterial, lipoxygenase and tyrosinase inhibition activities. Furthermore, cytocompatibility of the extract was also determined prior starting in vivo investigations. Then the in vivo performance of 2% bark extract loaded emulsion formulation was determined by using non-invasive probe cutometer and elastometer with comparison to base formulation. The preliminary experiment showed that bark extract has a significant amount of phenolic and flavonoid compounds with eminent antioxidant potential. Furthermore, indicated an efficient antibacterial, lipoxygenase, and tyrosinase enzyme inhibition activities. Importantly, the bark extract did not induce any toxicity or apoptosis, when incubated with HaCat cells. Moreover, the in vivo results showed the formulation (size 3 µm) decreased the skin melanin, erythema and sebum contents up to 2.1-,2.7-and 79%, while increased the skin hydration and elasticity up to 2-folds and 22% as compared to the base, respectively. Owing to enhanced therapeutic effects the phytocosmetic formulation proved to be a potential skin whitening, moisturizer, anti-acne, anti-wrinkle, anti-aging therapy and could actively induce skin rejuvenation and resurfacing.

Aglycone solanidine and solasodine derivatives: A natural approach towards cancer.

Over the past few years, it was suggested that a rational approach to treat cancer in clinical settings requires a multipronged approach that augments improvement in systemic efficiency along with modification in cellular phenotype leads to more efficient cell death response. Recently, the combinatory delivery of traditional chemotherapeutic drugs with natural compounds proved to be astonishing to deal with a variety of cancers, especially that are resistant to chemotherapeutic drugs. The natural compounds not only synergize the effects of chemotherapeutics but also minimize drug associated systemic toxicity. In this review, our primary focus was on antitumor effects of natural compounds. Previously, the drugs from natural sources are highly precise and safer than drugs of synthetic origins. Many natural compounds exhibit anti-cancer potentials by inducing apoptosis in different tumor models, in-vitro and in-vivo. Furthermore, natural compounds are also found equally useful in chemotherapeutic drug resistant tumors. Moreover, these Phyto-compounds also possess numerous other pharmacological properties such as antifungal, antimicrobial, antiprotozoal, and hepatoprotection. Aglycone solasodine and solanidine derivatives are the utmost important steroidal glycoalkaloids that are present in various Solanum species, are discussed here. These natural compounds are highly cytotoxic against different tumor cell lines. As the molecular weight is concerned; these are smaller molecular weight chemotherapeutic agents that induce cell death response by initiating apoptosis through both extrinsic and intrinsic pathways.