Nagarwal Ramesh Chand, Singh Paras Nath, Kant Shri, Maiti Pralay, Pandit Jayanta Kumar
Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, UP, India.
Chem Pharm Bull (Tokyo). 2011;59(2):272-8. doi: 10.1248/cpb.59.272.
The aim of this investigation was to develop 5-fluorouracil (5-FU) loaded chitosan nanoparticles (CH-DNPs) for ophthalmic delivery. CH-DNPs were fabricated by ionotropic gelation mechanism using chitosan (CH) and a polyanion (TPP). The nanoparticles were smooth and spherical, confirmed by scanning electron microscopy (SEM) and atomic force microscope (AFM). CH/TPP mass ratio and TPP significantly changed the particles size morphology and encapsulation efficiency. The nanoparticles size ranged from approximately 114 to 192 nm and had a positive zeta potential (30±4 mV). The encapsulation efficiency, loading capacity and recovery of DNPs were 8.12-34.32%, 3.14-15.24% and 24.22 to 67% respectively. Physical characterization was done by Fourier transform infrared (FT-IR) and X-ray diffraction (XRD). No interaction was observed in between drug and polymer and crystallinity of drug was not changed in drug loaded nanoparticles. In-vitro release study of DNPs showed diffusion controlled release. Bioavailability study of batch CS9 was studied in rabbit eye and compare to 5-FU solution. 5-FU level was significantly higher in aqueous humor of rabbit eye. Ocular tolerance was studied in the eye of New Zealand rabbits and tested formulation was non-irritant with no sign of inflammation.
本研究的目的是开发用于眼部给药的载有5-氟尿嘧啶（5-FU）的壳聚糖纳米粒（CH-DNPs）。采用壳聚糖（CH）和聚阴离子（TPP）通过离子凝胶化机制制备CH-DNPs。通过扫描电子显微镜（SEM）和原子力显微镜（AFM）证实纳米粒光滑且呈球形。CH/TPP质量比和TPP显著改变了颗粒大小、形态和包封率。纳米粒大小范围约为114至192 nm，具有正的zeta电位（30±4 mV）。DNPs的包封率、载药量和回收率分别为8.12 - 34.32%、3.14 - 15.24%和24.22至67%。通过傅里叶变换红外光谱（FT-IR）和X射线衍射（XRD）进行物理表征。未观察到药物与聚合物之间有相互作用，载药纳米粒中药物的结晶度未改变。DNPs的体外释放研究显示为扩散控制释放。对批次CS9进行了兔眼生物利用度研究，并与5-FU溶液进行比较。兔眼房水中5-FU水平显著更高。在新西兰兔眼中研究了眼耐受性，测试制剂无刺激性，无炎症迹象。
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