Université Paris-Sud 11, UMR CNRS 8612, Physicochimie - Pharmacotechnie - Biopharmacie, Faculté de Pharmacie, Châtenay-Malabry, France.
Eur J Pharm Biopharm. 2010 Oct;76(2):296-303. doi: 10.1016/j.ejpb.2010.07.004. Epub 2010 Jul 23.
The main objective of this work was to design thermosensitive and mucoadhesive vaginal hydrogels able to keep their rheological and mucoadhesive properties after dilution with vaginal fluids. Formulations were composed of pluronic F127 or a mix of two pluronics F127 and F68. Both formulations contained hydroxypropylmethyl cellulose (HPMC) as a mucoadhesive polymer. The determination of gelling temperature (T(gel)) after dilution with simulated vaginal fluid (SVF) demonstrated that hydrogels were resistant to dilution and T(gel) values were close to 30°C. Ex vivo mucoadhesion experiments conducted on porcine vaginal mucosa founded on the technique of traction of the adhesive/adherent joint allowed the characterization of mucoadhesive properties of hydrogels by measuring work of adhesion (W) and maximum force of detachment (F(max)). In the case of F127-based hydrogels, W and F(max) were lowered after dilution with SVF. However, in the case of F127/F68-based hydrogels, W, F(max) and mucoadhesion profiles were weakly affected by dilution. These differences could be attributed to the higher elasticity of F127/F68/HPMC (22.5/2.5/1% w/w) hydrogel in comparison with F127/HPMC one (20/1% w/w). Indeed, rheological analyses of the formulations showed that both elastic (G') and viscous moduli (G'') were higher for F127/F68/HPMC (22.5/2.5/1% w/w) than for F127/HPMC hydrogel (20/1% w/w). However, we demonstrated that the higher elasticity of the hydrogel was due to the higher total pluronic concentration and not due to the presence of F68 in the formulation.
这项工作的主要目的是设计热敏和黏膜粘附性阴道水凝胶，使其在与阴道液稀释后保持流变学和黏膜粘附性能。配方由泊洛沙姆 F127 或泊洛沙姆 F127 和 F68 的混合物组成。两种配方都包含羟丙基甲基纤维素 (HPMC) 作为黏膜粘附聚合物。用模拟阴道液 (SVF) 稀释后测定的凝胶化温度 (T(gel)) 表明，水凝胶能抵抗稀释，T(gel)值接近 30°C。在猪阴道黏膜上进行的基于牵引粘附/附着接头技术的体外黏膜粘附实验，允许通过测量粘附功 (W) 和最大分离力 (F(max)) 来表征水凝胶的黏膜粘附性能。在基于 F127 的水凝胶的情况下，W 和 F(max) 在与 SVF 稀释后降低。然而，在基于 F127/F68 的水凝胶的情况下，W、F(max) 和黏膜粘附特性受稀释的影响较小。这些差异可能归因于 F127/F68/HPMC(22.5/2.5/1%w/w)水凝胶的弹性高于 F127/HPMC 水凝胶(20/1%w/w)。实际上，配方的流变学分析表明，F127/F68/HPMC(22.5/2.5/1%w/w)水凝胶的弹性模量 (G') 和粘性模量 (G'') 均高于 F127/HPMC 水凝胶(20/1%w/w)。然而，我们证明水凝胶的高弹性归因于泊洛沙姆总浓度较高，而不是配方中存在 F68。
