Gonjari I D, Hosmani A H, Karmarkar A B, Godage A S, Kadam S B, Dhabale P N
Government College of Pharmacy, Satara, MS, India.
Drug Discov Ther. 2009 Feb;3(1):6-9.
The purpose of the present study was to develop ophthalmic gel formulations of fluconazole. Intraocular delivery of topically applied drugs such as fluconazole is hampered by elimination of the solution due to tear turnover, so an in situ gelling thermoreversible mucoadhesive gel was formulated. Thermoreversible mucoadhesive gels were prepared using the cold method along with poloxamer 407 and different mucoadhesive polymers such as hydroxy ethyl cellulose (HEC), hydroxy propyl methyl cellulose (HPMC) K4M, and polyvinyl pyrrolidone (PVP) K30. Gels were evaluated for physical parameters like appearance, gelation temperature, pH, spreadability, drug content, gel strength, bioadhesion, and in vitro permeation. A modified device (modified K-C diffusion cell with a sheep's eye corneal membrane as a diffusion membrane) was used for evaluation of drug permeation through a sheep's corneal membrane. The formulated gels were transparent, uniform in consistency, and had spreadability with a pH range of 6.8 to 7.3. Satisfactory bioadhesion on the sheep's corneal surface and good gel strength were also observed. Diffusion studies have shown that a matrix is the best-fit model. As the concentration of mucoadhesive agent increases, the rate of permeation decreases. The order of drug permeation through the membrane was HEC > PVP K30 > HPMC K4M. This study found that a thermoreversible polymer and mucoadhesive polymers can be effectively used to prolong residence time.
本研究的目的是开发氟康唑的眼用凝胶制剂。由于泪液周转会导致局部应用的药物（如氟康唑）溶液被清除，从而阻碍了其眼内递送，因此制备了一种原位凝胶化的热可逆粘膜粘附凝胶。采用冷法并使用泊洛沙姆407和不同的粘膜粘附聚合物（如羟乙基纤维素（HEC）、羟丙基甲基纤维素（HPMC）K4M和聚乙烯吡咯烷酮（PVP）K30）制备热可逆粘膜粘附凝胶。对凝胶的外观、凝胶化温度、pH值、铺展性、药物含量、凝胶强度、生物粘附性和体外渗透性等物理参数进行了评估。使用一种改良装置（以羊眼角膜作为扩散膜的改良K-C扩散池）来评估药物透过羊角膜的渗透性。所制备的凝胶是透明的，质地均匀，铺展性良好，pH值范围为6.8至7.3。还观察到在羊角膜表面具有令人满意的生物粘附性和良好的凝胶强度。扩散研究表明，基质是最佳拟合模型。随着粘膜粘附剂浓度的增加，渗透速率降低。药物透过膜的顺序为HEC > PVP K30 > HPMC K4M。本研究发现，热可逆聚合物和粘膜粘附聚合物可有效地用于延长滞留时间。
