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用于治疗痤疮的维甲酸负载立方液晶凝胶的制剂、体外和离体评价

Formulation, In-Vitro and Ex-Vivo Evaluation of Tretinoin Loaded Cubosomal Gel for the Treatment of Acne.

作者信息

Sureka Shruti, Gupta Gaurav, Agarwal Mohit, Mishra Anurag, K Singh Santosh, P Singh Ravindra, Sah Sushil K, de Jesus A Pinto Terezinha, Dua Kamal

机构信息

Department of Pharmaceutics, Smriti College of Pharmaceutical Education, Dewas Naka, Indore, Madhya Pradesh 452010, India.

Birat Medical College, Biratnagar, Nepal.

出版信息

Recent Pat Drug Deliv Formul. 2018;12(2):121-129. doi: 10.2174/1872211312666180213121117.

Abstract

OBJECTIVE

The current work was attempted to formulate and evaluate the topical sustained release delivery systems called cubosomes containing Tretinoin for the acne treatment. The recent patents on various formulations of tretinoin (EP0408370A2) helped in selecting a new formulation and evaluation.

METHODS

Tretinoin loaded cubosomes were prepared by bottom-up technique, using varying the concentration of lipid and surfactant and keeping the drug concentration constant, a total of nine formulations of tretinoin was developed. These preparations were evaluated for surface charge, particle size, particle morphology, encapsulation efficiency, in-vivo and in-vitro release studies of gel enriched with cubosome dispersion. Finally, the stability studies of cubosomal gel were performed on optimized formulations.

RESULTS

Significant result were obtained with tretinoin formulation as the drug is lipophilic, so it gives more depot effect on the epidermis and good retention property. The data obtained from the formulations showed that formulation TCF-5 was the optimized formulation which exhibited better drug release and entrapment efficiency.

CONCLUSION

It can be concluded that cubosomes offer benefits of quick onset as well as the maximal release of drug with fewer side effects. Thus, cubosomes represent a capable transporter having the property to sustain the release of drug, potential to localize the drug in the skin with a possible clinical application for acne vulgaris treatment due to cubosome depot effect on the epidermis.

摘要

目的

当前的工作旨在制备并评估一种名为立方液晶纳米粒的局部缓释给药系统,其载有维甲酸用于治疗痤疮。近期关于维甲酸各种制剂的专利(EP0408370A2)有助于选择新的制剂并进行评估。

方法

采用自下而上的技术制备载维甲酸的立方液晶纳米粒,通过改变脂质和表面活性剂的浓度并保持药物浓度恒定,共开发了九种维甲酸制剂。对这些制剂进行表面电荷、粒径、颗粒形态、包封率、富含立方液晶纳米粒分散体的凝胶的体内和体外释放研究。最后,对优化后的制剂进行立方液晶纳米粒凝胶的稳定性研究。

结果

维甲酸制剂取得了显著成果,由于该药物具有亲脂性,因此在表皮上具有更强的储库效应和良好的滞留性能。从这些制剂获得的数据表明,制剂TCF - 5是优化后的制剂,具有更好的药物释放和包封效率。

结论

可以得出结论,立方液晶纳米粒具有起效快以及药物最大释放且副作用较少的优点。因此,立方液晶纳米粒是一种有能力的转运体,具有维持药物释放的特性,由于其对表皮的储库效应,有可能将药物定位在皮肤中,在寻常痤疮治疗中具有潜在的临床应用价值。

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