Mehta Meenu, Dureja Harish, Garg Munish
a Department of Pharmaceutical Sciences , Maharshi Dayanand University , Rohtak , India.
Drug Deliv. 2016 Oct;23(8):3072-3081. doi: 10.3109/10717544.2016.1149744. Epub 2016 Mar 8.
Boswellic acids (BAs) are isolated from oleo gum of Boswellia serrata and are mainly used as potential anti-inflammatory, hypolipidemic, immunomodulatory, and antitumor agents. Pharmacokinetic investigations of BAs uncover its poor bioavailability through digestive system thus creates a need for improved therapeutic responses which can possibly be achieved by developing formulations through novel delivery system.
Present study was conducted to design topical BA-loaded proniosomal gel for the management of inflammatory disorders with enhanced bioavailability.
Nonionic surfactant vesicles were prepared using the coacervation phase separation method. A central composite design was employed to statistically optimize formulation variables using Design-Expert software. Three independent variables were evaluated: amount of surfactant (X), amount of soya lecithin (X), and amount of cholesterol (X). The encapsulation efficiency percentage (Y) and particle size (Y) were selected as dependent variables.
The optimum formulation (F10) displayed spherical bi-layered vesicles under transmission electron microscopy with optimum particle size of 707.9 nm and high entrapment efficiency as 98.52%. In vitro skin permeation study demonstrated the most sustained release of 84.83 ± 0.153 mg/cm in 24 h. Anti-inflammatory activity of the gel showed a significant (p < 0.001) higher percentage inhibition as compared to the marketed gel at the same dose.
The present study exhibited that BA-loaded proniosomal gel was better in terms of absorption, bioavailability, and release kinetics.
乳香酸(BAs)从乳香的油树脂中分离得到,主要用作潜在的抗炎、降血脂、免疫调节和抗肿瘤药物。对乳香酸的药代动力学研究发现其经消化系统的生物利用度较差,因此需要改进治疗反应,这可能通过新型给药系统开发制剂来实现。
开展本研究以设计用于治疗炎症性疾病的载乳香酸前体脂质体凝胶,提高其生物利用度。
采用凝聚相分离法制备非离子表面活性剂囊泡。采用中心复合设计,使用Design-Expert软件对制剂变量进行统计学优化。评估三个自变量:表面活性剂用量(X)、大豆卵磷脂用量(X)和胆固醇用量(X)。选择包封率百分比(Y)和粒径(Y)作为因变量。
最佳制剂(F10)在透射电子显微镜下显示为球形双层囊泡,最佳粒径为707.9nm,包封率高达98.52%。体外皮肤渗透研究表明,在24小时内释放最为持久,释放量为84.83±0.153mg/cm。该凝胶的抗炎活性在相同剂量下与市售凝胶相比,显示出显著更高的抑制百分比(p<0.001)。
本研究表明,载乳香酸前体脂质体凝胶在吸收、生物利用度和释放动力学方面表现更佳。