Application Of Topical Formulation Research Articles

Follicle-Targeted Delivery of Betamethasone and Minoxidil Co-Entrapped in Polymeric and Lipid Nanoparticles for Topical Alopecia Areata Treatment.

Alopecia areata is managed with oral corticosteroids, which has known side effects for patients. Given that a topical application of formulations containing a corticoid and a substance controlling hair loss progression could reduce or eliminate such adverse effects and increase the patient's adherence to the treatment, this study prepares polymeric and lipidic nanoparticles (PNPs and NLCs) to co-entrap minoxidil and betamethasone and compares the follicular drug delivery provided by topical application of these nanoparticles. The prepared PNPs loaded 99.1 ± 13.0% minoxidil and 70.2 ± 12.8% betamethasone, while the NLCs entrapped 99.4 ± 0.1 minoxidil and 80.7 ± 0.1% betamethasone. PNPs and NLCs presented diameters in the same range, varying from 414 ± 10 nm to 567 ± 30 nm. The thermal analysis revealed that the production conditions favor the solubilization of the drugs in the nanoparticles, preserving their stability. In in vitro permeation studies with porcine skin, PNPs provided a 2.6-fold increase in minoxidil penetration into the follicular casts compared to the control and no remarkable difference in terms of betamethasone; in contrast, NLCs provided a significant (specifically, a tenfold) increase in minoxidil penetration into the hair follicles compared to the control, and they delivered higher concentrations of betamethasone in hair follicles than both PNPs and the control. Neither PNPs nor NLCs promoted transdermal permeation of the drugs to the receptor solution, which should favor a topical therapy. Furthermore, both nanoparticles targeted approximately 50% of minoxidil delivery to the follicular casts and NLCs targeted 74% of betamethasone delivery to the hair follicles. In conclusion, PNPs and NLCs are promising drug delivery systems for enhancing follicular targeting of drugs, but NLCs showed superior performance for lipophilic drugs.

Protective effects of extracts from Acer truncatum leaves on SLS-induced HaCaT cells.

Introduction: A. truncatum Bunge (Sapindaceae or formerly Aceraceae) is a tall deciduous tree native to China. Traditionally, the leaves of A. truncatum are decocted and used by Chinese Mongolians, Koreans, and Tibetans to treat skin itching, dry cracks, and other skin ailments, which indicates A. truncatum leaves may have a potential inhibitory effect on various skin inflammations. Methods: To examine the protective effect against skin inflammations of A. truncatum leaf extract (ATLE), an in vitro dermatitis model was established using sodium dodecyl sulfate (SLS)-induced HaCaT cells. The anti-inflammatory effect of ATLE was evaluated by analyzing cell viability, apoptosis, reactive oxygen species (ROS), interleukin 6 (IL-6), and prostaglandin E2 (PGE2) levels. Results: Orthogonal experiments showed that the pretreatment with ATLE can reduce the IL-6 levels, PGE2 levels, and apoptosis increased in SLS-stimulated HaCaT cells, which indicates that ATLE has positive efficacy for dermatitis. Furthermore, three flavonoid compounds kaempferol-3-O-α-L-rhamnoside, quercetin-3-O-α-L-rhamnopyranoside, kaempferol-3,7-di-O-α-L-rhamnoside, and 1,2,3,4,6-Penta-O-galloyl-β-D-glucopyranose (PGG) were isolated and identified. Among them, kaempferol-3,7-di-O-α-L-rhamnoside was isolated from this plant for the first time. These compounds have been proven to have an anti-inflammatory effect. They may contribute to the efficacy of A. truncatumin treating skin inflammation. Discussion: The results revealed that ATLE has the potential to be used as an additive in various skin care products to prevent skin inflammations and may be incorporated in formulations for topical application as a therapeutic approach against dermatitis.

In vitro Kinetic Release Study, in vivo Hydration and Moisturizing Effect of Peel-off Oil-in-Water (O/W) Nanoemulsion Containing Kojic Monooleate for Topical Application

 A derivative of kojic acid, kojic monooleate (KMO) contains tyrosinase inhibitor, and exhibits strong antioxidant activity makes it a good candidate to be incorporated into a formulation for topical application. A peel-off was chosen to ensure a better hydration effect and permeability of KMO into the skin. The objectives of this research were to analyze the kinetic release study of peel-off oil-in-water O/W nanoemulsion containing KMO and evaluate the moisturizing and hydration effect towards human volunteers. The peel-off formulation was developed by adding 27.61% w/w polyvinyl alcohol (PVA) and 1.05% w/w propylene glycol (PG). The study was performed by using Franz cell, tewameter and corneometer to analyze the release rate of KMO from peel-off O/W nanoemulsion, moisturizing, and hydration effect of formulation towards humans after 180 min of application, respectively. The final formulation has a pH of 4.74, conductivity of 7.47 ± 4.05 x 10-3 microS/cm, viscosity 0.1058 Pa·s and spreadability of 61.86 ± 1.71 g·cm/s. It also disports 79.99 ± 2.53 % released of KMO across the cellulose acetate membrane after 180 min of study time.  The results of the hydration effect of the formulation towards human volunteers’ skin suggested that the peel-off O/W nanoemulsion containing KMO does increase the hydration of the skin by 12.33% due to the occlusive effect of KMO. In summary, this study presents new findings in kinetic release study, hydration and moisturizing effect of peel-off O/W nanoemulsion containing KMO for topical application.

Topical Ectoine Application in Children and Adults to Treat Inflammatory Diseases Associated with an Impaired Skin Barrier: A Systematic Review

IntroductionInflammatory skin diseases are a significant burden on affected patients. Inflammation is caused by various stress factors to the epidermis resulting in, e.g., dryness, redness, and pruritus. Emollients are used in basic therapy to restore the natural skin barrier and relieve symptoms. A systematic review was performed to evaluate the efficacy and safety of ectoine-containing topical formulations in inflammatory skin diseases characterized by an impaired skin barrier.MethodsA systematic review was carried out in PubMed, the Cochrane Library, and Microsoft Academic up to October 2021. Inclusion criteria were ectoine-containing topical formulations (creams, emollients) used for (adjuvant) therapy of inflammatory skin diseases. Clinical studies of any design published in any language were included.ResultsA total of 230 references were screened for eligibility, of which six were selected for inclusion in the review (five studies on atopic dermatitis and one study on prevention and management of retinoid dermatitis). The application of topical formulations containing 5.5–7.0% ectoine positively influenced skin dryness and, consequently, pruritus and dermatitis-specific scores in patients with atopic dermatitis. Especially in infants and children, who belong to the most frequently affected group, the formulations were well-tolerated when applied for up to 4 weeks. In studies where ectoine was used as an adjuvant therapy, application was associated with a decreased need for pharmacological therapy and also improved the effectiveness of, e.g., topical corticosteroids. In patients undergoing isotretinoin therapy, ectoine was as effective as dexpanthenol in reducing retinoid dermatitis or improving symptoms.ConclusionEctoine is an effective natural substance with an excellent tolerability and safety profile, representing a beneficial alternative as basic therapy or to increase the efficacy of the pharmacological treatment regimen for patients with inflammatory skin diseases, including infants and children.

IN-SITU FILM-FORMING SOLUTION FOR TOPICAL APPLICATION OF TERBINAFINE HCL: BIOPHARMACEUTICAL EVALUATION AND IN VIVO ANTIFUNGAL PERFORMANCE USING ANIMAL MODEL

Objective: The main purpose of this study is to develop a film-forming solution with optimum physical-mechanical characteristics and excellent antifungal activity to enhance deposition and penetration into the stratum corneum (SC). Methods: The film-forming solutions of terbinafine HCl were formulated using methacrylate copolymers, polyethylene glycol 400, and ethanol as diluent. The selected formulations were subjected to test of physical-mechanical properties, drug release, drug permeation across the stratum corneum and drug deposition study. The best formulation was further evaluated for in vivo antifungal efficacy. Results: The selected formulations exhibited superior pharmaceutical characteristics, including rapid drying, non-stickiness, and being transparency on the skin. Formulation A (FA) had significantly lower tensile strength (4.78 N/m2, p<0.05) and higher percentage elongation at break (33.61%, p<0.05), which reduced the firmness of the film, allowing it to be super-flexible in following the movement of the skin and preventing loss of film through abrasion. FA showed significantly (p<0.05) rapid drug permeation (1510.51 µg/cm2) across the stratum corneum (SC) at 24 h when compared with the other formulations and the positive control proprietary drug (PD), Terbex® cream formulation (475.8 µg/cm2). Conclusion: Having superior physical-mechanical and drug permeation characteristics, FA can be considered as an efficient, reproducible, and efficacious antifungal formulation for topical application.

The Silkworm as a Source of Natural Antimicrobial Preparations: Efficacy on Various Bacterial Strains.

The global spread of multi-resistant pathogens responsible for infections, which cannot be treated with existing drugs such as antibiotics, is of particular concern. Antibiotics are becoming increasingly ineffective and drug resistance is leading to more difficult-to-treat infections; therefore, new bioactive compounds with antimicrobial activity are needed and new alternative sources should be found. Antimicrobial peptides (AMPs) are synthesized by processes typical of the innate immune system and are present in almost all organisms. Insects are extremely resistant to bacterial infections as they can produce a wide range of AMPs, providing an effective first line of defense. The AMPs produced by insects therefore represent a possible source of natural antimicrobial molecules. In this paper, the possibility of using plasma preparations from silkworm (Bombyx mori) larvae as a source of antimicrobials was evaluated. After simple purification steps, insect plasma was analyzed and tested on different Gram-positive and Gram-negative bacterial strains. The results obtained are encouraging as the assays on Escherichia coli and Enterobacter cloacae showed significant decrease in the growth of these Gram-negative bacteria. Similar results were obtained on Gram-positive bacteria, such as Micrococcus luteus and Bacillus subtilis, which showed strong susceptibility to the silkworm AMPs pool. In contrast, Staphylococcus aureus displayed high resistance to Bombyx mori plasma. Finally, the tested plasma formulations were assessed for possible storage not only at 4 °C, but also above room temperature. In conclusion, partially purified plasma from silkworm could be a promising source of AMPs which could be used in formulations for topical applications, without additional and expensive purification steps.

Biotechnologically Produced Lavandula angustifolia Mill. Extract Rich in Rosmarinic Acid Resolves Psoriasis-Related Inflammation Through Janus Kinase/Signal Transducer and Activator of Transcription Signaling.

Psoriasis is a common skin pathology, characterized by dysregulation of epidermal keratinocyte function attended by persistent inflammation, suggesting that molecules with anti-inflammatory potential may be effective for its management. Rosmarinic acid (RA) is a natural bioactive molecule known to have an anti-inflammatory potential. Here we examined the effect of biotechnologically produced cell suspension extract of Lavandula angustifolia Mill (LV) high in RA content as treatment for psoriasis-associated inflammation in human keratinocytes. Regulatory genes from the nuclear factor kappa B (NF-κB) and Janus kinase/signal transducer and activator of transcription (JAK/STAT) signaling pathways were upregulated upon stimulation with a combination of interferon gamma (IFN-γ), interleukin (IL)-17A and IL-22. We also observed that both LV extract and RA could inhibit JAK2, leading to reduced STAT1 phosphorylation. Further, we demonstrated that LV extract inhibited phosphoinositide 3-kinases (PI3K) and protein kinase B (AKT), which could be implicated in reduced hyperproliferation in keratinocytes. Collectively, these findings indicate that the biotechnologically produced LV extract resolved psoriasis-like inflammation in human keratinocytes by interfering the JAK2/STAT1 signaling pathway and its effectiveness is due to its high content of RA (10%). Hence, both LV extract and pure RA possess the potential to be incorporated in formulations for topical application as therapeutic approach against psoriasis.

Epidermal Growth Factor in Aesthetics and Regenerative Medicine: Systematic Review.

Introduction:Epidermal Growth Factor (rhEGF) is a promising skin antiaging agent that successfully promotes skin wound repair, and it has been investigated in the past decade for these purposes. However, there are no updated systematic reviews, in English or English, that support the efficacy of rhEGF as a regenerative skin treatment or systematic reviews that compile the uses of rhEGF as facial aesthetic therapy and regenerative medicine.Aim:To describe the current state of facial aesthetic and regenerative medicine treatments in which rhEGF has been effectively used.Materials and Methods:An exhaustive search was carried out in “Medline” (via “PubMed”), “Cochrane,” “Bireme” through the Virtual Health Library (VHL), “Elsevier” via “Science Direct,” “Springer,” “SciELo,” “ResearchGate,” and Google Scholar. Studies related to the use of rhEGF in addressing skin disorders or skin aging are included.Results:Overall, 49 articles were found, which described the use of rhEGF for skin regeneration and restructuring. Efficacy in the regeneration of skin wounds was verified through the intradermal and topical application of formulations with rhEGF. Most clinical trials in aesthetics point to an effective inversion of skin aging. However, uncontrolled or randomized trials abound, so that does not represent enough evidence to establish its efficiency. There are transient adverse effects for both cases.Conclusion:The rhEGF considers an effective therapeutic alternative for patients with recalcitrant skin wounds and skin aging, as it is a potent and specific mitogenic factor for the skin.

Ferulic Acid Activity in Topical Formulations: Technological and Scientific Prospecting.

Ferulic acid is a phenolic compound widely distributed in monocotyledons, with several applications, especially in pharmaceutical and dermo-cosmetic industries. It has proven antioxidant and anti- inflammatory activities, among others, which are mainly ascribed to its molecular structure. The main factor that can lead to serious skin damages like inflammation, dryness, wrinkles, and cancer is the exposure to UV radiation that is responsible for an increased level of radical oxygen species. This review aims to evaluate the application of ferulic acid in topical formulations and the technologies used to enhance its bioavailability and stability, as well as to get a clearer picture of its effects by in vivo and in vitro studies. It covers technological publications in the WIPO, EPO, INPI, and USPTO databases and scientific publications in the PubMed, Web of Sciences, and Science Direct databases, exploring the trend and application of this compound by country and year of publication. Both the scientific and technological analyses showed the importance and tendency in the association of the Ferulic Acid and other vitamins and actives. The synergic effect certainly provides a better result, performance, and stability of the compounds, which cleared the great spectrum and applicability of the Ferulic Acid in topical formulations. The present literature survey revealed that ferulic acid exerts an important activity in several formulations for topical application and improved the stability and bioavailability when combined with new technologies and methods, showing an open path to target the treatment of skin disorders.

Topical application of a commercially available formulation of vitamin C stabilized by vitamin E and ferulic acid reduces tissue viability and protein synthesis in ex vivo human normal skin.

Aqueous formulations of vitamin C stabilized by vitamin E and ferulic acid at low pH effectively protect skin against reactive oxygen species-induced damage. However, the effects of these formulations on human skin have not clearly been described. The aim of this study was to investigate whether topical application of two commercially available formulations of vitamin C alter human skin using an ex vivo model. Human skin explants were topically treated on alternate days with commercially available formulation 1 (15% vitamin C) at 100% (without dilution), 50%, or 10% diluted in saline or formulation 2 (20% vitamin C) at 100% (without dilution), 50%, or 10% diluted in saline. Only saline was applied to control skin explants. Topical formulation 1 at 100%, 50%, or 10%, but not formulation 2 at 100%, 50%, or 10%, reduced the viability of ex vivo human skin compared to the control after 7, 10, and 13days. In addition, compared to the control, ex vivo human skin treated with formulation 1 at 50%, but not formulation 2 at 50%, also decreased mRNA levels of actin and ribosomal protein L10 and gene expression of extracellular matrix components after 10days. Furthermore, after 10days, topical application of formulation 1 at 50%, but not formulation 2 at 50%, decreased the protein expression of proliferating cellular nuclear antigen, lysyl oxidase, β-actin, and glyceraldehyde-3-phosphate dehydrogenase compared to the control. Topical formulation 1, but not formulation 2, may reduce the viability of and protein synthesis in ex vivo human skin. Those effects might be due to action of vehicle of formulation 1 on ex vivo human skin.

Melaleuca alternifolia Essential Oil: Evaluation of Skin Permeation and Distribution from Topical Formulations with a Solvent-Free Analytical Method.

Melaleuca alternifolia essential oil (tea tree oil) is widely used as an ingredient in skin care products because of its recognized biological activities. The European Scientific Committee on Consumer Products constantly promotes research and collection of data on both skin distribution and systemic exposure to tea tree oil components after the application of topical formulations. This study quantitatively evaluates permeation, skin layer distribution (stratum corneum, epidermis, and dermis), and release into the surrounding environment of bioactive tea tree oil markers (i.e., α-pinene, β-pinene, α-terpinene, 1,8-cineole, γ-terpinene, 4-terpineol, α-terpineol) when a 5% tea tree oil formulation is applied at a finite dosing regimen. Permeation kinetics were studied in vitro on pig ear skin using conventional static glass Franz diffusion cells and cells ad hoc modified to monitor the release of markers into the atmosphere. Formulation, receiving phases, and skin layers were analyzed using a fully automatic and solvent-free method based on headspace solid-phase microextraction/gas chromatography-mass spectrometry. This approach affords, for the first time, to quantify tea tree oil markers in the different skin layers while avoiding using solvents and overcoming the existing methods based on solvent extraction. The skin layers contained less than 1% of each tea tree oil marker in total. Only oxygenated terpenes significantly permeated across the skin, while hydrocarbons were only absorbed at trace level. Substantial amounts of markers were released into the atmosphere.

Topical delivery of niacinamide: Influence of neat solvents

Niacinamide (NIA) has been widely used in cosmetic and personal care formulations for several skin conditions. Permeation of topical NIA has been confirmed in a number of studies under infinite dose conditions. However, there is limited information in the literature regarding permeation of NIA following application of topical formulations in amounts that reflect the real-life use of such products by consumers. The aim of the present work was therefore to investigate skin delivery of NIA from single solvent systems in porcine skin under finite dose conditions. A secondary aim was to probe the processes underlying the previously reported low recovery of NIA following in vitro permeation and mass balance studies. The solubility and stability of NIA in various single solvent systems was examined. The solvents investigated included Transcutol® P (TC), propylene glycol (PG), 1-2 hexanediol (HEX), 1-2 pentanediol (1-2P), 1-5 pentanediol (1-5P), 1-3 butanediol (1-3B), glycerol (GLY) and dimethyl isosorbide (DMI). Skin permeation and deposition of the molecule was investigated in full thickness porcine skin in vitro finite dose Franz-type diffusion experiments followed by mass balance studies. Stability of NIA for 72h in the solvents was confirmed. The solubility of NIA in the solvents ranged from 82.9±0.8 to 311.9±4.5mg/mL. TC delivered the highest percentage permeation of NIA at 24h, 32.6±12.1% of the applied dose. Low total recovery of NIA after mass balance studies was observed for some vehicles, with values ranging from 55.2±12.8% to 106.3±2.3%. This reflected the formation of a number of NIA degradation by-products in the receptor phase during the permeation studies. Identification of other vehicles for synergistic enhancement of NIA skin delivery will be the subject of future work.

Topical Pilocarpine Formulation for Diagnosis of Cystic Fibrosis

Cystic fibrosis is diagnosed in infants by estimating the levels of chloride ions present in the sweat induced by iontophoresis of pilocarpine solution. Elevated levels of chloride (≥60 mMol/L) in sweat are indicative of cystic fibrosis. However, the iontophoretic method of delivering pilocarpine is cumbersome and usually is associated with several side effects such as skin burn, skin rashes, erythema, and so forth. The objective of this study was therefore to develop a topical formulation that delivers adequate amount of pilocarpine. The drug delivery of formulation was compared with iontophoresis of aqueous solution of pilocarpine nitrate in vitro using porcine skin model. The pilocarpine levels in the skin exposed to topical pilocarpine solution under mild hyperthermia was 152.04 ± 52.23 μg/cm2 after 10 min of application, whereas it was 97.05 ± 27.93 μg/cm2 in the skin after 10 min of iontophoresis. The topical formulation was subjected to clinical evaluation to assess the efficacy of the product to induce sweat production. The average amount of the sweat secreted on application of topical formulation was found to be 77.28 ± 18.97 mg. Based on these results, it was found that the topical formulation was successful in delivering pilocarpine and to stimulate sweat secretion.

Toxicological Evaluation of Some Essential Oils Obtained from Selected Romania Lamiaceae Species in Complex with Hydroxypropyl - gamma-cyclodextrin

Medicinal plants are highly investigated due to their multiple effects in human health. In the last two decades, plants belonging to Lamiaceae family have emerged as an important source of compounds with beneficial effects in various pathologies. Many species of the Lamiaceae family have a high volatile oil content which can be found in different parts of the plant. Some representative examples include Lavandula spp. Salvia spp. and Mentha spp. which are species with essential oils studied for antioxidant, antimicrobial and antitumor effects. The aim of this study was to evaluate the effect of six essential oils at skin level before and after encapsulation in hydroxypropyl-gamma-cyclodextrins. Results indicated that regardless of the tested form, the samples did not display an irritating or toxic effect at skin level, suggesting that the essential oils can be used in different formulations for topical application.

Toxicological Evaluation of Some Essential Oils Obtained from Selected Romania Lamiaceae Species in Complex with Hydroxypropyl - gamma-cyclodextrin

Medicinal plants are highly investigated due to their multiple effects in human health. In the last two decades, plants belonging to Lamiaceae family have emerged as an important source of compounds with beneficial effects in various pathologies. Many species of the Lamiaceae family have a high volatile oil content which can be found in different parts of the plant. Some representative examples include Lavandula spp. Salvia spp. and Mentha spp. which are species with essential oils studied for antioxidant, antimicrobial and antitumor effects. The aim of this study was to evaluate the effect of six essential oils at skin level before and after encapsulation in hydroxypropyl-gamma-cyclodextrins. Results indicated that regardless of the tested form, the samples did not display an irritating or toxic effect at skin level, suggesting that the essential oils can be used in different formulations for topical application. Keywords: essential oils, Lamiaceae, hydroxypropyl-gamma-cyclodextrins, mexametry, corneometry, tewametry

A modification for the calculation of water depth profiles in oil-treated skin by in vivo confocal Raman microscopy.

In this study, an extended calculation method for the determination of the water profiles in oil-treated skin is proposed, which is based on the calculation of the ratio between the Raman band intensities of water (3350-3550 cm-1 ) and keratin Amide I at 1650 cm-1 . The proposed method is compared with the conventional method based on the ratio of the Raman band intensities of water (3350-3550 cm-1 ) and keratin at 2930 cm-1 . The conventional method creates artifacts in the depth profiles of the water concentration in oil-treated skin, showing a lower amount of water in the upper and intermediate layers of the stratum corneum, which is due to the superposition of oil- and keratin-related Raman bands at 2930 cm-1 . The proposed extended method shows no artifacts and has the potential to determine the water depth profiles after topical application of formulations on the skin.

Polyoxazolines based mixed micelles as PEG free formulations for an effective quercetin antioxidant topical delivery.

This study aims to prove the value of the polyoxazolines polymer family as surfactant in formulations for topical application and as an alternative to PEG overuse. The amphiphilic polyoxazolines (POx) were demonstrated to have less impact on cell viability of mice fibroblasts (NIH3T3) than their PEG counterparts. Mixed micelles, made of POx and phosphatidylcholine, were manufactured using thin film and high pressure homogenizer process. The mixed micelles were optimized to produce nanosized vesicles of about 20 nm with a spherical shape and stable over 28 days. The natural lipophilic antioxidant, quercetin, was successfully encapsulated (encapsulation efficiency 94 ± 4% and drug loading 3.6 ± 0.2%) in the mixed micelles with no morphological variation. Once loaded in the formulation, the quercetin impact on cell viability of NIH3T3 was decreased while its antioxidant activity remained unchanged. This work highlights the capacity of amphiphilic POx to create, in association with phospholipids, stable nanoformulations which show promise for topical delivery of antioxidant and ensure skin protection against oxidative stress.

Isolation, Purification and Structural Identification of Degradation Products from Ketoconazole in a Liquid Formulation: An HPLC and HPLC-MS/MS Study

Ketoconazole is the active ingredient in an antifungal liquid formulation for topical application. A binary gradient HPLC analysis indicated that ketoconazole in the formulation produced four degradation products at minor levels after storage at room temperature for about 3 years.

Antibacterial hop extracts encapsulated in nanochitosan matrices

Hops and the components extracted from them are well known antibacterial agents used in beers and as food preservatives, in formulations for topical applications on their own or together with other antimicrobial agents, in hormone replacement therapy, as antioxidants, tumor development antagonists, and angiogenesis inhibitors. Their shortcomings: very low bioavailability, bitter taste, and susceptibility to oxidative decomposition have limited their applications. We propose nanosized chitosan, an inexpensive, readily available biopolymer with a broad spectrum of antibacterial activity, as carrier for lupulone (L) and xanthohumol (X), two components of hops. Chitosan nanoparticles (CNP) and chitosan-based nanocomposites encapsulating lupulone (CNL) and xanthohumol (CNX) were prepared by ionotropic gelation using sodium tripolyphosphate (TPP) as crosslinker. Different preparative ratios and conditions were investigated and the nanoparticles obtained were characterized by FTIR, colloidal titration, size, zeta potential, and antimicrobial activity. The kinetics of the release of L/X from composites was studied in vitro. All the nanoparticles were active against several Gram-positive, Gram-negative, and Candida strains. Synergistic interactions were observed in all cases, although hops are known mainly for their activity against Gram-positive bacteria. All nanoparticles showed good stability over several months.

A Novel Topical Spray Formulation for Ginkgo Bioloba for Antifungal Activity

The aim of this study is to prove the antifungal and antibacterial activity of Ginko Biloba GKB from glycerin nanocapsules and nanoemulsions. GKB was formulated as spray formulation for topical application using ethyl alcohol 95%/glycerol/water based formulations. GKB spray was evaluated for their particle size distribution, pH, content uniformity, content per spray, in vitro release and antifungal activity. The antifungal activity determined by Agar well-diffusion method. The formulae were tested for their skin permeation and the stability of the formulations. The results showed uniform formulae with nano-sized particles, pH compatible with the topical formulation and higher drug content. Diffusion studies of the optimized formulations through the abdominal rabbit skin showed higher penetrated drug over a period of 24 h. Stability studies indicated that formulations were stable. Skin irritation studies confirmed the compatibility of spray formulae with skin. Agar well-diffusion method showed that GKB was effective compared with fluconazole. The inhibition zones for all formulae were significant as compared with standard fluconazole. The results obtained showed that the topical spray formulation could be a promising and innovative therapeutic system as topical antifungal for the transdermal administration of GKB. The developed formulation can be used for delivery from spray formulation. This study proved the local activity of GKB as antifungal drugs.