Influence of Bile Acids in Hydrogel Pharmaceutical Formulations on Dissolution Rate and Permeation of Clindamycin Hydrochloride

Clindamycin hydrochloride is a widely used antibiotic for topical use, but its main disadvantage is poor skin penetration. Therefore, new approaches in the development of clindamycin topical formulations are of great importance. We aimed to investigate the effects of the type of gelling agent (carbomer and sodium carmellose), and the type and concentration of bile acids as penetration enhancers (0.1% and 0.5% of cholic and deoxycholic acid), on clindamycin release rate and permeation in a cellulose membrane in vitro model. Eight clindamycin hydrogel formulations were prepared using a 23 full factorial design, and they were evaluated for physical appearance, pH, drug content, drug release, and permeability parameters. Although formulations with carbomer as the gelling agent exerted optimal sensory properties, carmellose sodium hydrogels had significantly higher release rates and permeation of clindamycin hydrochloride. The bile acid enhancement factors were higher in carbomer gels, and cholic acid exerted more pronounced permeation-enhancing effects. Since the differences in the permeation parameters of hydrogels containing cholic acid in different concentrations were insignificant, its addition in a lower concentration is more favorable. The hydrogel containing carmellose sodium as a gelling agent and 0.1% cholic acid as a penetration enhancer can be considered as the formulation of choice.

Effect of Manufacturing and Absorption Promotion of Lidocaine Hydrogel Using Ultrasonic Waves during Cosmetic Procedures

Purpose: In this study, we study to more effectively use anesthesia products used in beauty procedures following the popularization of anti-aging. Hydrogel, which contains lidocaine, is believed to be more effective in relieving pain if used in cosmetic procedures with ultrasonic waves.Methods: The availability of manufactured hydrogels and commercial gels for ultrasonic treatment was compared, and the effect on skin penetration and skin penetration due to ultrasonic limitations was evaluated based on their applicability. Usability and optimal ultrasound parameters were identified during ultrasound treatment.Results: Viscosity measurement, gelation rate, swelling, skin permeability experiment, and HPLC analysis of manufactured hydrogels all revealed properties, with skin permeability being highest at frequency 1 MHz, cycle low 200, and high 50.Conclusions: Finally, hydrogels containing lidocaine increased skin permeability during ultrasound treatment, allowing for faster targeted transdermal transmission that was more effective depending on the ultrasound parameters. As a result, it is determined that it can be used in cosmetic procedures.

A Review on Chemical Permeation Enhancers used in the Formulation of Transdermal Drug Delivery System

Skin penetration enhancement technology is a rapidly evolving area that will greatly increase the quantity of transdermal drug delivery medications. Penetration enhancers are used to facilitate the movement of drugs through the skin barrier. Numerous methods exist for extending partition enhancement. The enhancers' contact with the polar head of the lipid groups is the potential means for increasing the penetration. Penetration enhancers improve the amount of free water molecules between the bilayer, leading to an improvement of the polar drug diffusion cross section. This article focuses on the different compounds assessed for improving penetration activity like sulphoxides, azones, pyrrolidones, alcohols and alkanols, glycols, surfactants and terpenes.

Transdermal Drug delivery: A step towards treatment of cancer

Background: Transdermal drug delivery is an emerging and tempting system over oral and hypodermic drug delivery system. With the new developments in skin penetration techniques, anticancer drugs ranging from hydrophilic macromolecules to lipophilic drugs can be administered via transdermal route to treat cancer. Objective: In the present review, various approaches to enhance the transdermal delivery of drugs is discussed including the micro and nanotechnology based transdermal formulations like chemotherapy, gene therapy, immunotherapy, phototherapy, vaccines and medical devices. Limitations and advantages of various transdermal technologies is also elaborated. Method: In this review, patent applications and recent literature of transdermal drug delivery systems employed to cure mainly cancer are covered. Results: Transdermal drug delivery systems have proved their potential to cure cancer. They increase the bioavailability of drug by site specific drug delivery and can reduce the side effects/toxicity associated with anticancer drugs. Conclusion: The potential of transdermal drug delivery systems to carry the drug may unclutter novel ways for therapeutic intercessions in various tumors.

Epilobium angustifolium L. Essential Oil—Biological Activity and Enhancement of the Skin Penetration of Drugs—In Vitro Study

Epilobium angustifolium L. is a popular medicinal plant found in many regions of the world. This plant contains small amounts of essential oil whose composition and properties have not been extensively investigated. There are few reports in the literature on the antioxidant and antifungal properties of this essential oil and the possibility of applying it as a potential promoter of the skin penetration of drugs. The essential oil was obtained by distillation using a Clavenger type apparatus. The chemical composition was analyzed by the GC-MS method. The major active compounds of E. angustifolium L. essential oil (EOEa) were terpenes, including α-caryophyllene oxide, eucalyptol, β-linalool, camphor, (S)-carvone, and β-caryophyllene. The analyzed essential oil was also characterized by antioxidant activity amounting to 78% RSA (Radical Scavenging Activity). Antifungal activity against the strains Aspergillus niger, A. ochraceus, A. parasiticum, and Penicillium cyclopium was also determined. The largest inhibition zone was observed for strains from the Aspergillus group. The EOEa enhanced the percutaneous penetration of ibuprofen and lidocaine. After a 24 h test, the content of terpene in the skin and the acceptor fluid was examined. It has been shown that the main compounds contained in the essential oil do not penetrate through the skin, but accumulate in it. Additionally, FTIR-ATR analysis showed a disturbance of the stratum corneum (SC) lipids caused by the essential oil application. Due to its rich composition and high biological activity, EOEa may be a potential candidate to be applied, for example, in the pharmaceutical or cosmetic industries. Moreover, due to the reaction of the essential oil components with SC lipids, the EOEa could be an effective permeation enhancer of topically applied hydrophilic and lipophilic drugs.

Multipotentiality of Luliconazole against Various Fungal Strains: Novel Topical Formulations and Patent Review

Background: Luliconazole is a broad-spectrum antifungal agent with impactful fungicidal and fungistatic activity. It has shown exceptional potency against miscellaneous fungal strains like Candida, Aspergillus, Malassezia, Fusarium species and various dermatophytes. Objective: Luliconazole belongs to class Ⅱ of the Biopharmaceutical Classification System with low aqueous solubility. Although it is available conventionally as 1% w/v topical cream, it has limitations of lower skin permeation and shorter skin retention. Therefore, nanoformulations based on various polymers and nanostructure carriers can be employed to overcome the impediments regarding topical delivery and efficacy of luliconazole. Methods: In this review, we have tried to provide insight into the literature gathered from authentic web resources and research articles regarding recent research conducted on the subject of formulation development, patents, and future research requisites of luliconazole. Results: Nanoformulations can play a fundamental role in improving topical delivery by escalating dermal localization and skin penetration. Fabricating luliconazole into nanoformulations can overcome the drawbacks and can efficiently enhance its antimycotic activity. Conclusion: It has been concluded that luliconazole has exceptional potential in the treatment of various fungal infections, and therefore, it should be exploited to its maximum for its innovative application in the field of mycology.

Permeability of Ibuprofen in the Form of Free Acid and Salts of L-Valine Alkyl Esters from a Hydrogel Formulation through Strat-M™ Membrane and Human Skin

This paper aimed to evaluate the effect of vehicle and chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen [IBU]. In vitro permeation experiments were performed using human abdominal skin and Strat-M™ membrane. The HPLC method was used for quantitative determinations. The formulations tested were hydrogels containing IBU and its derivatives and commercial gel with ibuprofen. The results obtained indicate that Celugel® had an enhancing effect on the skin penetration of IBU. The average cumulative mass of [IBU] after 24 h permeation test from Celugel® formulation through human skin was over 3 times higher than for the commercial product. Three ibuprofen derivatives containing [ValOiPr][IBU], [ValOPr][IBU], and [ValOBu][IBU] cation were evaluated as chemical penetration enhancers. The cumulative mass after 24 h of penetration was 790.526 ± 41.426, 682.201 ± 29.910, and 684.538 ± 5.599 μg IBU cm−2, respectively, compared to the formulation containing unmodified IBU-429.672 ± 60.151 μg IBU cm−2. This study demonstrates the perspective of the transdermal hydrogel vehicle in conjunction with the modification of the drug as a potential faster drug delivery system.

Transfersomes as alternative topical nanodosage forms for the treatment of skin disorders

Topical drug delivery is a promising approach to treat different skin disorders. However, it remains a challenge mainly due to the nature and rigidity of the nanosystems, which limit deep skin penetration, and the unsuccessful demonstration of clinical benefits; greater penetration by itself, does not ensure pharmacological success. In this context, transfersomes have appeared as promising nanosystems; deformability, their unique characteristic, allows them to pass through the epidermal microenvironment, improving the skin drug delivery. This review focuses on the comparison of transfersomes with other nanosystems (e.g., liposomes), discusses recent therapeutic applications for the topical treatment of different skin disorders and highlights the need for further studies to demonstrate significant clinical benefits of transfersomes compared with conventional therapies.