Joshi Monika, Sharma Vijay, Pathak Kamla
Department of Pharmaceutics, Rajiv Academy for Pharmacy, N.H.# 2, Delhi Mathura Road, P.O. Chhatikkara, Mathura 281001, India.
Department of Pharmaceutics, Rajiv Academy for Pharmacy, N.H.# 2, Delhi Mathura Road, P.O. Chhatikkara, Mathura 281001, India.
Int J Pharm. 2015 Jan 15;478(1):268-277. doi: 10.1016/j.ijpharm.2014.11.050. Epub 2014 Nov 25.
The project was aimed at development of isotretinoin nail lacquer and assessment of its penetration efficiency across human nail plate. Preliminary studies (hydration enhancement factor and SEM) aided the selection of thioglycolic acid as permeation and eugenol was selected as local anesthetic in the formulation. The nail lacquer was optimized by 3(2) factorial design and a total of nine formulations were prepared and screened. In vitro adhesion and ex vivo permeation (cumulative drug permeation per unit area (CDP/A) = 6.61 ± 0.57 mg/cm(2)) across bovine hoof guided the selection of F3 as optimized formulation that was improvised. Viscosity adjustments to improve handling characteristics were affected by incorporation of ethyl cellulose (6%; F3M1) that scaled the viscosity to 312.681 cp and insignificantly (p > 0.05) affected CDP/A (6.32 ± 0.45 mg/cm(2)). In comparison to marketed preparation (Retino-A cream) F3M1 afforded two fold increase in CDP/A. The permeation characteristics were defined by Higuchi model (r(2) = 0.964) and flux value of 176 μg/cm(2)/h. Confocal laser scanning microscopy, after 72 h of nail lacquer application, revealed extensive distribution of the fluorescent tracer across the human nail plate in comparison to control that was confined to the top layer. Conclusively, an efficacious and stable nail lacquer of isotretinoin was developed for potential clinical topical use to target the drug to nail bed in treatment of nail psoriasis.
该项目旨在开发异维A酸指甲油,并评估其穿透人指甲板的效率。初步研究(水合增强因子和扫描电子显微镜)有助于选择巯基乙酸作为渗透剂,丁香酚被选为制剂中的局部麻醉剂。通过3(2)析因设计优化指甲油,共制备并筛选了9种制剂。体外附着力和在牛蹄上的离体渗透(单位面积累积药物渗透量(CDP/A)=6.61±0.57mg/cm²)指导了F3作为优化制剂的选择,该制剂进行了改进。通过加入乙基纤维素(6%;F3M1)来调整粘度以改善操作特性,其将粘度调整至312.681厘泊,对CDP/A(6.32±0.45mg/cm²)的影响不显著(p>0.05)。与市售制剂(维甲酸乳膏)相比,F3M1的CDP/A提高了两倍。渗透特性由Higuchi模型(r²=0.964)和通量值176μg/cm²/h定义。在涂抹指甲油72小时后,共聚焦激光扫描显微镜显示,与仅局限于顶层的对照相比,荧光示踪剂在人指甲板上广泛分布。总之,开发了一种有效且稳定的异维A酸指甲油,用于潜在的临床局部应用,以在治疗甲银屑病时将药物靶向甲床。