Developing the Potential Ophthalmic Applications of Pilocarpine Entrapped Into Polyvinylpyrrolidone-Poly(acrylic acid) Nanogel Dispersions Prepared By γ Radiation
Developing the Potential Ophthalmic Applications of Pilocarpine Entrapped Into Polyvinylpyrrolidone-Poly(acrylic acid) Nanogel Dispersions Prepared By γ Radiation
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DOI：
10.1021/bm301742m
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发表时间：
2013-03-01
影响因子：
6.2
通讯作者：
Hamed, Ashraf A.
中科院分区：
文献类型：
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作者：
Abd El-Rehim, Hassan A.;Swilem, Ahmed E.;Hamed, Ashraf A.
本研究的目的是提高匹罗卡品的稳定性和生物利用度，以便在作用部位长时间保持足够的浓度。因此，以聚乙烯吡咯烷酮（PVP）为模板聚合物，在丙烯酸（AAc）水溶液中通过伽马辐射诱导聚合制备ph敏感型聚乙烯吡咯烷酮聚丙烯酸（PVP/PAAc）纳米凝胶，用于包封匹罗卡品。通过对影响粒径和包封效率的因素进行优化，获得了适合于高效包封药物的纳米凝胶。采用动态光散射（DLS）、ζ电位（zeta potential）、傅里叶红外光谱（FTIR）和透射电镜（TEM）对PVP/PAAc纳米凝胶颗粒进行了表征，结果表明，PVP/PAAc纳米凝胶颗粒的大小可由原料组成、浓度和辐照剂量控制。通过静电相互作用将匹罗卡品装入纳米凝胶颗粒中，富aac纳米凝胶的负载效率最高。研究了纳米凝胶的透光性、黏附性和流变性，以评价其在眼内的适用性。在模拟泪液中进行的体外释放研究表明，与溶液中的匹罗卡品相比，所制备的PVP/PAAc纳米凝胶颗粒的匹罗卡品的持续释放时间相对较长。
The aim of this study was to improve the stability and bioavailability of pilocarpine in order to maintain an adequate concentration of the pilocarpine at the site of action for prolonged period of time. Thus, pH-sensitive polyvinylpyrrolidone poly-(acrylic acid) (PVP/PAAc) nanogels prepared by gamma radiationinduced polymerization of acrylic acid (AAc) in an aqueous solution of polyvinylpyrrolidone (PVP) as a template polymer were used to encapsulate pilocarpine. Factors affecting size and encapsulation efficiency were optimized to obtain nanogel suitable for entrapping drug efficiently. The PVP/PAAc nanogel particles were characterized by dynamic light scattering (DLS), zeta potential, Fourier transform infrared spectroscopy (FTIR), and transmission electron microscopy (TEM), and their size can be controlled by the feed composition and concentration as well as the irradiation dose. Pilocarpine was loaded into the nanogel particles through electrostatic interactions where the AAc-rich nanogels exhibited the highest loading efficiency. The transmittance, mucoadhesion, and rheological characteristics of the nanogel particles Were studied to evaluate their ocular applicability. The in vitro release study conducted in simulated tear fluid showed a relatively long sustained release of Pilocarpine from the prepared PVP/PAAc nanogel particles if compared with pilocarpine in solution.