Formulation and Evaluation of Valproic Acid Microemulsions for Enhanced Transfollicular Delivery in Guinea Pig Skin.

IF 2.3 4区 医学 Q2 DERMATOLOGY Journal of Cosmetic Dermatology Pub Date : 2024-11-20 DOI:10.1111/jocd.16685
Anayatollah Salimi, Soroush Jafarian, Arghavan Salimi, Saeed Mohammad Soleymani
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Abstract

Background: Valproic acid (VPA) is used to treat various neurological and psychiatric conditions. While oral VPA can cause hair loss, topical application has shown potential for hair regeneration. This study aimed to develop and evaluate microemulsion (ME) formulations of VPA for enhanced transfollicular delivery.

Methods: VPA-loaded MEs were prepared using oleic acid, Transcutol P, Tween 80, Labrasol, and Capryol 90. The MEs were characterized for physicochemical properties, stability, in vitro release, and ex vivo permeation through the hairy abdominal and nonhairy ear skin of guinea pigs.

Results: Eight stable ME formulations were developed with droplet sizes ranging from 10 to 24 nm, pH 4.6 to 5.2, and viscosity 77 to 85 cps. In vitro release studies showed controlled release profiles over 24 h. Permeation studies revealed enhanced drug delivery through both follicular and nonfollicular pathways compared with aqueous VPA solution. Formulations with higher surfactant/cosurfactant ratios showed increased permeation through the follicular pathway.

Conclusion: The ME formulations significantly enhanced VPA penetration into both epidermal and follicular pathways compared with aqueous solution. The composition of the MEs, particularly the oil content, water content, and surfactant/cosurfactant ratio, played a crucial role in determining the physicochemical properties and skin permeation parameters of VPA.

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丙戊酸微乳剂的配制与评估,用于增强在豚鼠皮肤中的经叶脉给药。
背景:丙戊酸(VPA)用于治疗各种神经和精神疾病。虽然口服 VPA 会导致脱发,但局部应用已显示出毛发再生的潜力。本研究旨在开发和评估VPA的微乳剂(ME)配方,以增强经毛囊给药:方法:使用油酸、Transcutol P、Tween 80、Labrasol 和 Capryol 90 制备了负载 VPA 的微乳剂。方法:使用油酸、Transcutol P、Tween 80、Labrasol 和 Capryol 90 制备了载入 VPA 的 ME,并对这些 ME 的理化性质、稳定性、体外释放以及通过豚鼠有毛腹部皮肤和无毛耳部皮肤的体内外渗透进行了表征:结果:研制出了八种稳定的 ME 配方,液滴大小为 10 至 24 纳米,pH 值为 4.6 至 5.2,粘度为 77 至 85 cps。与 VPA 水溶液相比,渗透研究显示通过滤泡和非滤泡途径的药物输送均有所增强。表面活性剂/共表面活性剂比率较高的制剂通过毛囊途径的渗透性更强:结论:与水溶液相比,ME 配方能明显提高 VPA 在表皮和毛囊途径中的渗透率。ME 的成分,尤其是油含量、水含量和表面活性剂/共表面活性剂的比例,在决定 VPA 的理化特性和皮肤渗透参数方面起着至关重要的作用。
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来源期刊
CiteScore
4.30
自引率
13.00%
发文量
818
审稿时长
>12 weeks
期刊介绍: The Journal of Cosmetic Dermatology publishes high quality, peer-reviewed articles on all aspects of cosmetic dermatology with the aim to foster the highest standards of patient care in cosmetic dermatology. Published quarterly, the Journal of Cosmetic Dermatology facilitates continuing professional development and provides a forum for the exchange of scientific research and innovative techniques. The scope of coverage includes, but will not be limited to: healthy skin; skin maintenance; ageing skin; photodamage and photoprotection; rejuvenation; biochemistry, endocrinology and neuroimmunology of healthy skin; imaging; skin measurement; quality of life; skin types; sensitive skin; rosacea and acne; sebum; sweat; fat; phlebology; hair conservation, restoration and removal; nails and nail surgery; pigment; psychological and medicolegal issues; retinoids; cosmetic chemistry; dermopharmacy; cosmeceuticals; toiletries; striae; cellulite; cosmetic dermatological surgery; blepharoplasty; liposuction; surgical complications; botulinum; fillers, peels and dermabrasion; local and tumescent anaesthesia; electrosurgery; lasers, including laser physics, laser research and safety, vascular lasers, pigment lasers, hair removal lasers, tattoo removal lasers, resurfacing lasers, dermal remodelling lasers and laser complications.
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