Development Of Topical Formulation Research Articles

Herbal Innovations in Eczema Care: A Comprehensive Review of Formulation Development, Safety, and Efficacy

Eczema, also known as atopic dermatitis, presents a significant challenge in clinical management due to its multifactorial etiology and variable clinical manifestations. Conventional treatments often focus on symptom relief and inflammation control, yet concerns regarding their long-term safety and efficacy persist. In recent years, there has been growing interest in exploring herbal therapies as adjunctive or alternative treatments for eczema management. This review aims to provide a comprehensive overview of the development and evaluation of topical herbal formulations specifically targeted at managing infectious eczema. Beginning with an introduction to eczema, encompassing its prevalence, underlying pathophysiology, and conventional treatment modalities, the review sets the stage for exploring the potential of herbal therapies. It delves into the significance of herbal treatments in eczema care, emphasizing their potential advantages such as efficacy, safety, and patient acceptability. The review then outlines the systematic approach to formulation development, encompassing the selection of herbal ingredients, optimization of base formulations, and rigorous stability testing. Safety evaluation strategies, including toxicological assessments, skin irritation potential, and allergenicity testing, are discussed to ensure the safety and tolerability of the herbal formulations. Efficacy evaluation involves assessing anti-inflammatory properties, antimicrobial activity, and conducting well-controlled clinical trials to determine their clinical efficacy and impact on patient outcomes. Through a comprehensive discussion and analysis, this review aims to elucidate the potential of topical herbal formulations as promising therapeutic options for managing infectious eczema, while also identifying areas for further research and optimization

Cutaneous targets for topical pain medications in patients with neuropathic pain: individual differential expression of biomarkers supports the need for personalized medicine.

Numerous potential cutaneous targets exist for treating chronic pain with topically applied active pharmaceutical ingredients. This preliminary human skin tissue investigation was undertaken to characterize several key biomarkers in keratinocytes and provide proof-of-principle data to support clinical development of topical compounded formulations for peripheral neuropathic pain syndromes, such as postherpetic neuralgia (PHN). The study intended to identify objective biomarkers in PHN skin on a patient-by-patient personalized medicine platform. The totality of biopsy biomarker data can provide a tissue basis for directing individualized compounded topical preparations to optimize treatment efficacy. Referencing 5 of the most common actives used in topical pain relief formulations (ketamine, gabapentin, clonidine, baclofen, and lidocaine), and 3 well-established cutaneous mediators (ie, neuropeptides, cannabinoids, and vanilloids), comprehensive immunolabeling was used to quantify receptor biomarkers in skin biopsy samples taken from ipsilateral (pain) and contralateral (nonpain) dermatomes of patients with PHN. Epidermal keratinocyte labeling patterns were significantly different among the cohort for each biomarker, consistent with potential mechanisms of action among keratinocytes. Importantly, the total biomarker panel indicates that the enriched PHN cohort contains distinct subgroups. The heterogeneity of the cohort differences may explain studies that have not shown statistical group benefit from topically administered compounded therapies. Rather, the essential need for individual tissue biomarker evaluations is evident, particularly as a means to direct a more accurately targeted topical personalized medicine approach and generate positive clinical results.

Development and Validation of a Chromatographic Method for Ibrutinib Determination in Human and Porcine Skin

Ibrutinib (IBR) is a tyrosine kinase inhibitor investigated for treating solid and non-solid tumors. Considering the advantages that a topical application of IBR could generate in terms of dose reduction and side effects in skin cancer treatment, this paper presents a simple and selective HPLC method for determining IBR concentration in in vitro skin permeation studies to support the development of topical formulations. The method uses a reversed-phase C18 column and a mobile phase composed of acetonitrile and 0.01 mol/L phosphoric acid at pH 3.5 (35:65 v/v), flowing at 1.0 mL/min. The oven temperature was set at 35 °C, the injection volume was 20 μL, and UV drug detection was performed at 259 nm. The validation procedure certified that this method was selective for IBR determination even when extracted from human or porcine skin matrices. The method was linear over a range of 0.2 to 15.0 μg/mL, precise, robust, and accurate, with recovery rates from the skin layers higher than 89.5 ± 5.9% for the porcine skin and higher than 92.0 ± 0.2% for the human skin. The limits of detection and quantification were 0.01 and 0.02 μg/mL, respectively. The method showed, therefore, to be adequate for use in further skin permeation studies employing IBR topical formulations.

Rational development of topical climbazole formulations

Dandruff, or pityriasis capitis simplex, is a common scalp condition associated with excessive flaking and scaling of the epidermal tissue. Other features include irregular corneocyte turnover, irritation, itching and an impaired skin barrier function. Previously we reported the characterization of climbazole (CBZ), an antifungal agent used in the management of dandruff. Skin permeation of CBZ from neat solvents was also investigated. In the present work we evaluated CBZ permeation in human skin in vitro from more complex formulations that better represent products used by consumers. The various systems studied were composed of propylene glycol (PG), Transcutol®P (TC), octyl salicylate (OSal) and isopropyl alcohol (IPA). As well as measurement of skin uptake and penetration of CBZ, where possible, the skin retention and permeation of the various solvents was also determined. All vehicles promoted skin permeation of CBZ but no significant differences in amount permeated were evident between the binary vehicles (PG:TC, TC:OSal) and the ternary vehicle studied (PG:IPA:OSal). The binary vehicles generally promoted more skin uptake of CBZ compared with the neat solvents (PG, TC, OSal) studied previously. Permeation and skin extraction of CBZ from the PG:TC vehicles increased with increasing PG content; a similar trend was evident for the PG:IPA:OSal systems. New methods were developed and validated for measurement of PG, TC and OSal. Analysis of the individual solvents indicated that PG permeation was also independent of the amounts of other solvents in the binary or ternary systems. Consistent with previous findings higher proportions of TC permeated compared with PG for the PG:TC binary systems; TC also permeated the skin more rapidly than PG from these vehicles. For OSal, skin extraction was generally higher for TC:OSal compared with the PG:IPA:OSal vehicle. However, increasing the content of OSal did not appear to influence CBZ skin uptake nor permeation. Interestingly, the effects of the various PG:TC vehicles on CBZ skin delivery contrast with results we previous reported for the same systems for a different active. This confirms that with reference to skin permeation, formulation effects and/or skin penetration enhancement should be expected to vary and may not be predicted for specific vehicles.

Potential Effects of Essential Oil from Plinia cauliflora (Mart.) Kausel on Leishmania: In Vivo, In Vitro, and In Silico Approaches.

In the search for new chemotherapeutic alternatives for cutaneous leishmaniasis (CL), essential oils are promising due to their diverse biological potential. In this study, we aimed to investigate the chemical composition and leishmanicidal and anti-inflammatory potential of the essential oil isolated from the leaves of Plinia cauliflora (PCEO). The chemical composition of PCEO showed β-cis-Caryophyllene (24.4%), epi-γ-Eudesmol (8%), 2-Naphthalenemethanol[decahydro-alpha] (8%), and trans-Calamenene (6.6%) as its major constituents. Our results showed that the PCEO has moderate cytotoxicity (CC50) of 137.4 and 143.7 μg/mL on mice peritoneal exudate cells (mPEC) and Vero cells, respectively. The PCEO was able to significantly decrease mPEC infection by Leishmania amazonensis and Leishmania braziliensis. The value of the inhibitory concentration (IC50) on amastigote forms was about 7.3 µg/mL (L. amazonensis) and 7.2 µg/mL (L. braziliensis). We showed that PCEO induced drastic ultrastructural changes in both species of Leishmania and had a high selectivity index (SI) > 18. The in silico ADMET analysis pointed out that PCEO can be used for the development of oral and/or topical formulation in the treatment of CL. In addition, we also demonstrated the in vivo anti-inflammatory effect, with a 95% reduction in paw edema and a decrease by at least 21.4% in migration immune cells in animals treated with 50 mg/kg of PCEO. Taken together, our results demonstrate that PCEO is a promising topical therapeutic agent against CL.

Evaluation of Antioxidants’ Ability to Enhance Hyaluronic Acid-Based Topical Moisturizers

Introduction: Hyaluronic acid (HA) is a unique molecule with multiple biological activities. In skin, HA plays an essential role as a humectant, capable of binding up to 1000 times its mass with water, leading to both skin moisturization and extracellular matrix rigidity. HA concentration and synthesis decreases significantly in aging skin, due to exogenous and endogenous factors, including photoaging and HA metabolism, respectively. A key driver for HA degradation and decrease in concentration is mediated via the induction of reactive oxygen species (ROS) and other free radicals. In this study, we evaluate antioxidant ingredients essential in the development of next-generation multi-weight HA-based topical formulations aimed at leveraging hyaluronic acid’s ability to maximize anti-aging properties. Methods: Two antioxidants, glycine saponin and glycyrrhetinic acid, were evaluated for stimulation of endogenous HA production and inhibition of endogenous hyaluronidase activity in an in vitro and cell-free assay. Results: The antioxidant glycine saponin induced endogenous HA synthesis in keratinocytes, while the antioxidant glycyrrhetinic acid demonstrated an approximately 54% reduction of hyaluronidase activity for the HA-degrading enzyme HYAL1. Conclusion: This study demonstrates the ability of two antioxidants (glycine saponin and glycyrrhetinic acid, essential in the development of the next generation of multi-weight HA plus antioxidant complex-based topical skin formulations) to limit the signs of aging skin, addressing limitations of many currently available topical HA-based formulations.

Development of Topical Formulations Containing 20% of Coated and Uncoated Zinc Oxide Nanoparticles: Stability Assessment and Penetration Evaluation by Reflectance Confocal Laser Microscopy

The introduction of zinc oxide nanoparticles (ZnOn) in sunscreens solved the issue of poor spreadability of these formulations, which often left a white film on the skin. However, safety concerns have arisen regarding the topical application of ZnOn. Some studies employed commercial sunscreens to address the safety issues of the topical application of ZnOn; however, commercial formulations are often complex and contain a wide range of ingredients that could attenuate the potential damage caused by the ZnOn. Therefore, in this study we aimed to develop a simple stable formulation containing 20% of coated and uncoated ZnOn, characterize the formulations and the nanoparticles, and assess the skin penetration in a Franz diffusion cell. The Feret’s diameter for the uncoated and coated ZnOn was 137 nm and 134 nm, respectively. For the uncoated ZnOn the hydrodynamic size in water was 368 nm and for the coated ZnOn, the average hydrodynamic size in ethyl acetate was 135 nm. The incorporation of ZnOn led to formulations more consistent and easier to spread, as suggested by the lower work of shear and higher values of firmness, cohesiveness, consistency and index of viscosity compared with the vehicle. The stability assessment at 45 °C suggested that the formulations containing the ZnOn were stable for 30 days and the vehicle was stable for 90 days. The assessment of the skin penetration by reflectance confocal laser microscopy indicated that the ZnOn did not permeate into the deepest layers of the skin, but accumulated on the skin furrows, hair and hair follicles.

Development of novel topical cosmeceutical formulations with antimicrobial activity against acne-causing microorganisms from <em>Coriandrum sativum</em> L.

Spices possess a diverse array of natural phytochemicals with antibacterial, anti-inflammatory, and antioxidant effects. Hence spices could be employed to treat chronic dermatologic conditions like acne vulgaris which involves infection of Propionibacterium acnes and Staphylococcus aureus, and inflammation. Particularly with the emergence of antibiotic resistance, there is an utmost necessity for the development of novel therapeutic agents for the management of acne. Thus, this study was focused on the development of novel topical gel formulations from the seeds of Coriandrum sativum L. (coriander) and to evaluate the antibacterial potential against some acne-causing bacterial species. Initially, the antibacterial effects of the n-hexane, ethyl acetate, and methanol extracts were screened against S. aureus and P. acnes by agar well diffusion assay. Thereafter, ethyl acetate extract of C. sativum was incorporated at predetermined three different concentrations into a novel topical gel base. Agar well diffusion assay and the broth microdilution method were used to evaluate the antibacterial activity of the resulting formulations. Interestingly, all three formulations inhibited the growth of P. acnes and S. aureus, with the highest activity in the formulation comprised of 15% w/w of the seed extract. Furthermore, the antibacterial activity and physical parameters like pH, color, and consistency of these formulations were retained during the storage period of 30 days, demonstrating their suitability as effective therapeutic alternatives in the management of acne vulgaris.

Electrospun PCL/PVA Coaxial Nanofibers with Embedded Titanium Dioxide and Magnetic Nanoparticles for Stabilization and Controlled Release of Dithranol for Therapy of Psoriasis

Dithranol is one of the oldest and most efficient drugs used in the treatment of psoriasis. One of the challenges with using dithranol is its photostability, because it easily degrades when exposed to light. This study investigated the potential of coaxial core-sheath PCL/PVA nanofibers as a dual-functional system for enhancing dithranol photostability and remote-controlled drug delivery for psoriasis therapy. We have shown that coaxial nanofibers with titanium oxide nanoparticles (reflecting and absorbing ultra-violet light) in the PVA-based sheath part of the nanofibers can increase dithranol photostability. Incorporation of dithranol and magnetic nanoparticles into a PCL-based core of the nanofibers enables dithranol release control via an external radio-frequency field. The application of a radio-frequency field generates heat that can be used to control the release rate of drugs. Our approach therefore offers a non-invasive and remotely controlled drug release system that hold promise for the development of new topical formulations for psoriasis treatment using dithranol.

Photochemoprevention of topical formulation containing purified fraction of Inga edulis leaves extract.

Natural antioxidants have attracted attention for their therapeutic use as photochemopreventive agents. Inga edulis leaves extract and its purified fraction have high polyphenolic content and high antioxidant capacity. In addition, they presented UV photostability and low citotoxicity in fibroblast cells. In this context, this study first aimed at development of topical formulation containing purified fraction of I. edulis extract and the evaluation of skin penetration of the compounds. Moreover, the photoprotective/photochemopreventive potential of the formulation containing I. edulis purified fraction were investigated in vitro and in vivo. The topical formulation containing 1% of the purified fraction of I. edulis increased the endogenous antioxidant potential of the skin, and vicenin-2 and myricetin compounds were able to penetrate the epidermis and dermis. Additionally, the purified fraction (25 and 50 mg/mL) showed a photoprotective effect against UVA and UVB radiation in L929 fibroblast cells. In vivo studies have shown that the formulation added with purified fraction provided an anti-inflammatory effect on the skin of animals after UVB exposure, since it was observed a reduction in MPO activity, IL-1β and TNF-α cytokines, and CXCL1/KC chemokine concentrations. In conclusion, the purified fraction of I. edulis, rich in phenolic compounds, when incorporated in topical formulation, appears as an alternative to prevent skin damages induced by UV radiation, due to its antioxidant and anti-inflammatory properties.

Development and in vitro assessment of Analgesic and Anti-inflammatory Mefenamic acid Nanosponge Loaded Topical Formulation

The present research work was done with the objective of topical formulation development of poorly water-soluble drug Mefenamic acid. The drug was firstly incorporated in nanosponge of ethyl cellulose. Then Mefenamic acid nanosponge-loaded topical gel formulations were developed by using Carbopol 934 as a gel-forming polymer. The Mefenamic acid-loaded nanosponges were tested for various quality parameters such as particle size distribution, polydispersity.index(PI),. Surface morphology and drug entrapment efficiency etc. Gel formulations were tested for viscosity, pH, in vitro diffusion and other parameters. The average size of developed nanosponge preparations was found between 250nm to 894nm. Scanning electron microscopy photographs of developed formulations clearly reveal the spongy and porous nature of particles along with spherical shape. The PI was. found in. the range. of 0.206 to 0.934. It was found that formulation N3 with a drug-to-polymer ratio of 1:4 has the highest drug loading. Further nanosponge were characterized for different parameters and results revealed acceptable characteristics of N3 formulation. These prepared nanosponges were loaded in topical Carbopol gel (Formulation G3) and evaluated for in vitro diffusion release. Obtained in vitro data was applied to numerous kinetic models which reveal typical zero order in vitro drug diffusion with prolonged release of Mefenamic acid and therefore it can be effectively used as analgesic and anti-inflammatory formulation.

Characterization of piroctone olamine for topical delivery to the skin.

Dandruff and its more severe related condition, seborrheic dermatitis affects a high proportion of the population at some point in their life. Piroctone olamine, also known as Octopirox® (OPX) is the monoethanolamine salt of piroctone and is an antifungal agent widely used for the management of dandruff. The aim of the present work was to characterize the physicochemical properties of piroctone olamine and to conduct pre-formulation studies for the development of novel topical formulations of this active. An HPLC method was developed and validated for the analysis of OPX. The melting point was determined using the DSC Q2000 (TA Instruments, USA). The distribution coefficient (logD(O/PBS) ) and partition coefficient (log Po/w ) was determined in phosphate-buffered saline (PBS) AND deionized (DI) water using the shake flask method. All experiments were performed at room temperature. The solubility was determined experimentally by adding amount of active to a solvent. The samples were kept at 32° ± 1°C for 48 h in a water bath. The stability of the compound was determined in a range of solvents by preparing solutions of 1mg mL-1 in the relevant solvents. These solutions were kept and stirred throughout the experiment at 32 ± 1°C, and aliquots were taken at 24, 48 and 96 h. The HPLC method was developed successfully; however, samples at the lower end of the calibration curve showed lower degrees of precision and accuracy. Based on experiments with DSC, the melting point was observed at an onset temperature of 132.4°C. The LogD was determined to be 1.84. The compound had the highest solubility in methanol (278.4mg mL-1 ) and propylene glycol (PG), with a value of 248.8mg mL-1 . The lowest solubility for OPX was in dimethyl isosorbide (9.9mg mL-1 ), Labrafac™ (3.6mg mL-1 ) and isostearyl isostearate (0.5mg mL-1 ). Over the 4 days, OPX showed stability in ethanol and PG, while a notable decrease in OPX was observed in PBS and DI water at 32 ± 1°C. The physicochemical properties of OPX were characterized to find suitable excipients able to target the epidermis for topical delivery. Building on these findings, future work will focus on the development of novel topical formulation of OPX.

Methodology of the Development of a Topical Transdermal Fucoidan Delivery System

Introduction. Marine-derived polysaccharides are promising candidates for the development of innovative drugs. One of such compounds is the polysaccharide fucoidan from brown seaweeds, which shows anticoagulant and anti-inflammatory activity. The development of topical transdermal formulation for the treatment of chronic venous diseases is of particular interest, because with targeted delivery, the active compound in high concentration comes directly to the site where the drug is required, while the risk of side effects is minimal.Aim. Experimental and theoretical justification of the methodological scheme for the development of a transdermal delivery system with fucoidan for local therapy using the Quality by Design (QbD) approach.Materials and methods. Fucoidan was isolated from the thalli of Fucus vesiculosus L. from the Barents Sea according to the original technology of the MMBI RAS. All excipients were approved for medical use. The experiments for rational selection of the excipients for the transdermal delivery system (TSD) were planned using the Greek-Latin square 4 × 4 with repeated observations. The colloidal and thermal stability and pH were evaluated as physicochemical parameters of TSD Structural and mechanical properties of TSD were deter-mined with rotational viscometer. The dissolution rate of fucoidan in vitro was evaluated using the paddle-over-disk method at a temperature of 32 ± 0.5 °C.Results and discussion. The composition and technology of topical TSD цwith fucoidan were developed using the QbD concept. The composition and technology of topical TSD with 15 % of fucoidan as active ingredient were developed. TSD has thermo- and colloidal stability, and has a pH value close to the pH of human skin. Poloxamer 407 was used as a gel base; olive oil was used as a hydrophobic phase. It was found that the ratio of poloxamer 407 to the aqueous phase should be no less than 0.1 and no more than 0.37; the ratio of water to the aqueous phase should not be less than 0.56 and not more than 0.69; and the ratio of polyoxyl 40 hydrogenated castor oil to the oil phase must be at least 0.34. It was found that 9 % poloxamer 407 provides the necessary structural and mechanical properties of TSD. It has been established that the developed TSD of fucoidan with poloxamer 407 belongs to non-Newtonian flow types with plastic properties and has thixotropy.Conclusion. The complex of studies based on QbD approach led to the experimental and theoretical justification of the methodological scheme for the development of a transdermal delivery system with marine polysaccharide fucoidan. The methodological scheme takes into account the physicochemical and technological features of fucoidan and allows you to create a high-quality TSD that ensures stability and complete release of the active substance.

Potential of Icariin–Glucosamine Combination in the Treatment of Osteoarthritis by Topical Application: Development of Topical Formulation and In Vitro Permeation Study

The aim of this study was to develop a topically applied formulation with the potential to alleviate arthritis ailments. A combination of two active ingredients, icariin from Epimedium L. (Species: Epimedium Koreanum) extract as a potential promoter of chondrogenesis and glucosamine sulfate as a precursor of cartilage tissues, was tested. In permeation studies, the potential for skin permeation of both substances was confirmed; however, the in vitro release test did not accurately reflect the degree of skin permeation. The in vitro release of icariin was at a level of 15.0–19.0% for the plant-extract-derived icariin and 29.0–35.0% for the pure substance. The level of glucosamine sulfate release was 38.4% (on average). For icariin of both origins, the release results were higher than those obtained via oral administration (about 12.0%), which shows the potential superiority of topical application. In addition, the physicochemical parameters that affect the in vitro release and performance of topical formulations were addressed. This preliminary research and permeation analysis of the formulation produced a promising picture of its prospects regarding arthritis treatment, although further investigation is needed.

A comparative study of the in vitro permeation of 2-phenoxyethanol in the skin PAMPA model and mammalian skin

For permeation studies that use excised skin, experimental data may show variability associated with the use of biological tissues. As a consequence, achieving reproducible results and data interpretation may be challenging. The skin parallel artificial membrane permeability assay (skin PAMPA) model has been proposed as a high-throughput tool for predicting skin permeation of chemicals. A number of skin cleansing wipe formulations for the diaper area of infants contain 2-phenoxyethanol (PE) as a preservative and cetylpyridinium chloride (CPC) as a surfactant with antimicrobial activity. However, information regarding cutaneous absorption of PE and CPC in the scientific literatures is remarkably limited. The main aim of the present study was to assess the suitability of the skin PAMPA model for prediction of skin permeation of PE. A secondary aim was to investigate the influence of CPC on the dermal absorption of PE. PE (1 % w/w) was prepared in two vehicles, namely propylene glycol (PG) and water-PG (WP). Permeability of PE was investigated in vitro using the skin PAMPA membrane, porcine skin and human skin under finite dose conditions. The highest permeation of PE was observed for the water-PG preparation with 0.2 % w/w of CPC. This finding was consistently observed in the skin PAMPA model and in Franz cell studies using porcine skin and human skin. Permeation of CPC was not detected in the three permeation models. However, permeation of PE increased significantly (p < 0.05) in the presence of CPC compared with formulations without CPC. When comparing the skin PAMPA data and the mammalian skin data for the cumulative amount of PE permeated, the r2 values for PAMPA-porcine skin and PAMPA-human skin were 0.84 and 0.89, respectively. The findings in this study demonstrate the capability of the skin PAMPA model to differentiate between various doses and formulations and are encouraging for further applications of this model as a high throughput screening tool in topical formulation development.

The Use of Proteins, Lipids, and Carbohydrates in the Management of Wounds

Despite the fact that skin has a stronger potential to regenerate than other tissues, wounds have become a serious healthcare issue. Much effort has been focused on developing efficient therapeutical approaches, especially biological ones. This paper presents a comprehensive review on the wound healing process, the classification of wounds, and the particular characteristics of each phase of the repair process. We also highlight characteristics of the normal process and those involved in impaired wound healing, specifically in the case of infected wounds. The treatments discussed here include proteins, lipids, and carbohydrates. Proteins are important actors mediating interactions between cells and between them and the extracellular matrix, which are essential interactions for the healing process. Different strategies involving biopolymers, blends, nanotools, and immobilizing systems have been studied against infected wounds. Lipids of animal, mineral, and mainly vegetable origin have been used in the development of topical biocompatible formulations, since their healing, antimicrobial, and anti-inflammatory properties are interesting for wound healing. Vegetable oils, polymeric films, lipid nanoparticles, and lipid-based drug delivery systems have been reported as promising approaches in managing skin wounds. Carbohydrate-based formulations as blends, hydrogels, and nanocomposites, have also been reported as promising healing, antimicrobial, and modulatory agents for wound management.

Development and Optimization of Erythromycin Loaded Transethosomes Cinnamon Oil Based Emulgel for Antimicrobial Efficiency

Erythromycin (EM) is a macrolide antibiotic that is frequently used to treat skin bacterial infections. It has a short half-life (1-1.5 h), instability in stomach pH, and a low oral bioavailability. These foregoing factors limit its oral application; therefore, the development of topical formulations loaded with erythromycin is an essential point to maximize the drug's concentration at the skin. Accordingly, the current study's goal was to boost the antimicrobial activity of EM by utilizing the advantages of natural oils such as cinnamon oil. Erythromycin-loaded transethosomes (EM-TE) were generated and optimized using a Box-Behnken design employing, phospholipid concentration (A), surfactant concentration (B), and ethanol content (C) as independent variables. Their effects on entrapment efficiency, EE, (Y1) and the total amount of erythromycin that penetrated the skin after 6 h, Q6h (Y2), were assessed. The optimized transethosome showed a particle size of 256.2 nm, EE of 67.96 ± 0.59%, and Q6h of 665.96 ± 5.87 (µg/cm2) after 6 h. The TEM analysis revealed that, the vesicles are well-known packed structures with a spherical shape. The optimized transethosomes formulation was further transformed into a cinnamon oil-based emulgel system using HPMC as a gelling agent. The generated EM-TE-emulgel was characterized by its physical features, in vitro, ex vivo studies, and antimicrobial activities. The formulation showed sufficient characteristics for effective topical application, and demonstrated a great stability. Additionally, EM-TE-Emulgel had the highest transdermal flux (120.19 μg/cm2·h), and showed considerably (p < 0.05) greater antimicrobial activity, than EM-TE-gel and placebo TE-Emulgel. The action of EM was subsequently augmented with cinnamon oil, which eventually showed a notable effect against bacterial growth. Finally, these results demonstrate that the transethosomes-loaded cinnamon oil-based emulgel is an alternative way to deliver erythromycin for the treatment of topical bacterial infections.

Curcumin quantification in skin and mucosa: Optimization of extraction and chromatographic method validation

Curcumin is a natural phenol found in the rhizome of Curcuma longa. It has been studied to treat several human carcinomas, such as melanomas and breast, head and neck, prostate, and ovary cancers. Here, we develop and validate a method for recovering curcumin from the skin layers and mucosa and selectively quantifying it, aiming to support permeation studies in developing topical formulations containing the natural compound. Recovery of curcumin from the stratum corneum, remaining skin, and mucosa was performed using ethanol, DMSO/ethanol, and DMSO, respectively, under mild stirring for specific periods. The separation of curcumin from the other curcuminoids, skin, and mucosa interferents was obtained using a C18 column as a stationary phase. The mobile phase was composed of pH 3.0 phosphoric acid at 1.0 mmol/L and acetonitrile (47:53, v/v), which flowed at 1 mL min−1. UV–Vis detection of curcumin was at 424 nm. The chromatographic method was selective, linear (r > 0.999), with a regression curve in the concentration range from 1.0 to 30.0 μg mL−1, robust, precise, and accurate, with curcumin recovery rates higher than 95 ± 7 % from the mucosa, 82 ± 2 % from the stratum corneum, and 65 ± 10 % from the remaining skin. Finally, the method was successfully used in a skin permeation test performed with porcine skin and mucosa. The validated method is, therefore, suitable for the recovery and quantification of curcumin from the skin layers and mucosa, favoring the development of new topical formulations destined for these sites of administration.

Formulation of Topical Itraconazole Nanostructured Lipid Carriers (Nlc) Gel for Onychomycosis

Itraconazole is a triazole antifungal agent that is synthesised. Itraconazole has been manufactured into a variety of pharmacological formulations and administered by a variety of ways. Itraconazole pills are used to treat pulmonary fungal infections that can spread throughout the body. Because Itraconazole is not yet officially listed in any pharmacopoeia, only a few procedures for quality control and stability testing in pharmaceutical formulations have been published. The development of itraconazole-loaded nanostructured lipid carriers (ITZ-NLC). Itraconazole NLC have been successfully developed. Itraconazole topical NLC developed for the treatment of onychomycosis does not exist, according to my survey.The development and evaluation of stable itraconazole topical gel formulations proved successful. Itraconazole NLC was produced utilising the microemulsion method, indicating the viability of adopting this method as a continuous manufacturing tool for NLC formulation. Further, the ITZ- NLC was incorporated in the gelling agent and we evaluated it under specific parameters.

Phase equilibrium, dynamics and rheology of phospholipid-ethanol mixtures: a combined molecular dynamics, NMR and viscometry study.

Binary mixtures of ethanol and phospholipids DOPC and DOPE have been investigated in a composition range relevant for topical drug delivery applications. This was done using a combined computer simulation and experimental approach where molecular dynamics simulations of ethanol-lipid mixtures with different compositions were performed. Several key properties including diffusion coefficients, longitudinal relaxation times, and shear viscosity were computed. In addition, diffusion coefficients, viscosities and NMR longitudinal relaxation times were measured experimentally for comparison and in order to validate the results from simulation. Diffusion coefficients and relaxation times obtained from simulations are in good agreement with results from NMR and computed viscosities are in reasonable agreement with viscometry experiments indicating that the simulations provide a realistic description of the ethanol-phospholipid mixtures. Structural changes in the simulated systems were investigated using an analysis based on radial distribution functions. This showed that the structure of ethanol-DOPC mixtures remains essentially unchanged in the investigated concentration range while ethanol-DOPE mixtures undergo structural rearrangements with the tendency for forming small aggregates on the 100 ns time scale consisting of less than 10 lipids. Although our simulations and experiments indicate that no larger aggregates form, they also show that DOPE has stronger aggregation tendency than DOPC. This highlights the importance of the character of the lipid headgroup for lipid aggregation in ethanol and gives new insights into phase equilibrium, dynamics and rheology that could be valuable for the development of advanced topical drug delivery formulations.