YANG Wen-yu, JIANG Chun-yan, YAN Dong, et al. Development of Resveratrol Nasal Gel Using Tibetan Hulless Barley -glucan as a Matrix[J]. Chinese journal of experimental traditional medical formulae, 2011, 17(12): 6-11.
DOI:
YANG Wen-yu, JIANG Chun-yan, YAN Dong, et al. Development of Resveratrol Nasal Gel Using Tibetan Hulless Barley -glucan as a Matrix[J]. Chinese journal of experimental traditional medical formulae, 2011, 17(12): 6-11. DOI: CNKI:11-3495/R.20110420.0932.010.
Development of Resveratrol Nasal Gel Using Tibetan Hulless Barley -glucan as a Matrix
并用多个药物释放数学模型探讨该凝胶剂的体外释放和渗透鼻黏膜的机制。 结果: 凝胶强度和黏度等参数的测定结果表明该凝胶剂具有柔软、易涂展、持水性好、黏度大但呈假塑性流动、黏附性好、pH与鼻腔pH相近等特点;体外试验8 h
累积释放度和渗透猪鼻黏膜累积透过率分别为93.86%
62.46%
释药机制均符合Weibull模型。 结论: 白藜芦醇青稞β-葡聚糖凝胶剂对鼻腔黏膜有很好的相容性
并具有良好的黏附和释药性能
用特制鼻腔给药装置可实现给药方便性。
Abstract
Objective: Tibetan hulless barley β-glucan (THBG) is a natural bioadhesive material. The present study was aimed at developing a THBG-based mucoadhesive gel of resveratrol
a potential cancer therapeutic agent richly obtained from the roots of Polyclonum cuspidatum and some other traditional Chinese medicines with low oral bioavailability
for nasal systemic delivery. Method: A 2% resveratrol nasal gel was prepared with 4% THBG as a matrix and 1% menthol as a penetrant
and characterized in terms of its physical properties (including pH
viscosity
gel strength
water holding capacity and mucoadhesion)
in vitro cumulative release and in vitro transmucosal cumulative delivery in porcine olfactorymucosa. The administration convenience of a specially designed controllable nasal injector and mucosa irritancy of the selected gel were also evaluated in healthy volunteers. Result: The nasal gel was found to exhibit pseudoplastic rheology with properties of high viscosity
low gel strength
high water holding capacity
strong mucoadhesion
good spreadability
easy administration and no irritation. The percents of cumulative release in vitro and transmucosal cumulative delivery in vitro at 8h were 93.86% and 62.46% respectively
and the drug release behavior in two tests were observed to fit the Weibull distribution model well. Conclusion: The results demonstrated that the THBG-based nasal gel of resveratrol is a patient-friendly dosage form with desirable bioadhesion
distribution
and release performance
and the THBG is suitable for using as the matrix of mucoadhesive preparations.