Patel Mrunali Rashmin, Patel Rashmin Bharatbhai, Parikh Jolly R, Patel Bharat G
a Department of Pharmaceutics and Pharmaceutical Technology , Indukaka Ipcowala College of Pharmacy , New Vallabh Vidyanagar , Gujarat , India.
b Department of Pharmaceutical Chemistry and Quality Assurance and.
Pharm Dev Technol. 2016 Dec;21(8):921-932. doi: 10.3109/10837450.2015.1081610. Epub 2015 Aug 31.
The objective of this study was to develop and evaluate a novel microemulsion based gel formulation containing tazarotene for targeted topical therapy of acne. Psudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant, and co-surfactant for microemulsion formation. The optimized microemulsion formulation containing 0.05% tazarotene was formulated by spontaneous microemulsification method consisting of 10% Labrafac CC, mixed emulsifiers 15% Labrasol-Cremophor-RH 40 (1:1), 15% Capmul MCM, and 60% distilled water (w/w) as an external phase. All plain and tazarotene-loaded microemulsions were clear and showed physicochemical parameters for desired topical delivery and stability. The permeation profiles of tazarotene through rat skin from optimized microemulsion formulation followed the Higuchi model for controlled permeation. Microemulsion-based gel was prepared by incorporating Carbopol®971P NF in optimized microemulsion formulation having suitable skin permeation rate and skin uptake. Microemulsion-based gel showed desired physicochemical parameters and demonstrated advantage over marketed formulation in improving the skin tolerability of tazarotene indicating its potential in improving its topical delivery. The developed microemulsion-based gel may be a potential drug delivery vehicle for targeted topical delivery of tazarotene in the treatment of acne.
本研究的目的是开发并评估一种新型的含他扎罗汀的微乳基凝胶制剂，用于痤疮的靶向局部治疗。构建伪三元相图以获得形成微乳所需的油、表面活性剂和助表面活性剂的浓度范围。通过自发微乳化法制备了含0.05%他扎罗汀的优化微乳制剂，其由10%的Labrafac CC、15%的混合乳化剂Labrasol-Cremophor-RH 40（1:1）、15%的Capmul MCM和60%的蒸馏水（w/w）作为外相组成。所有普通微乳和载他扎罗汀微乳均澄清，且显示出符合理想局部给药和稳定性要求的物理化学参数。他扎罗汀从优化微乳制剂透过大鼠皮肤的渗透曲线符合Higuchi控释渗透模型。通过在具有合适皮肤渗透率和皮肤摄取率的优化微乳制剂中加入Carbopol®971P NF制备微乳基凝胶。微乳基凝胶显示出理想的物理化学参数，并且在改善他扎罗汀的皮肤耐受性方面优于市售制剂，表明其在改善局部给药方面的潜力。所开发的微乳基凝胶可能是一种潜在的药物递送载体，用于他扎罗汀在痤疮治疗中的靶向局部递送。
