Preparation and Drug Release Study of Novel Nanopharmaceuticals with Polysorbate 80 Surface Adsorption

Xiaojun Tao,Jiajin Yi,Yu Li,Li Zhu,Xing Feng,Jianzhuo Hu,Zixuan Huang,Qian Hu,Xiaoping Yang

doi:10.1155/2018/4718045

Abstract

Most free drugs that cross the blood–brain barrier are characterized by high liposolubility, but they often have limited clinical applications because of poor dissolution and poor bioavailability. In this study, we prepared donepezil drug-loaded nanoparticles (DZP) with cholesterol-modified pullulan (CHP) as the nanocarrier (DZP-CHP) and surface modified the drug-loaded nanoparticles to improve the water solubility of donepezil while enhancing its targeting and sustained release. We determined the drug loading and encapsulation efficiency of DZP-CHP nanoparticles at different feed ratios. The mean ± SD drug loading and entrapment efficiency were high: 13.52 ± 2.03 and 86.54 ± 1.31. On dynamic light-scattering measurement, mean ± SD particle size was 260.7 ± 1.76 nm, polydispersity index 0.123 ± 0.004, and zeta potential −5.75 ± 0.64 mV. DZP-CHP nanoparticles prepared with the optimal feed ratio (DZP : CHP = 1 : 5) were coated with polysorbate 80, and the adsorption process was determined by isothermal titration calorimetry. We found good affinity between polysorbate 80 and DZP-CHP, with mean ± SD coverage 2.7 ± 0.372. The mean ± SD drug loading and entrapment efficiency of polysorbate 80-emulsified DZP-CHP nanoparticles were 8.25 ± 1.80 and 91.28 ± 4.57, respectively, and the proportion of drug released by 72 h was 42.71%. Compared to DZP-CHP alone, PS-DZP-CHP can enhance the release of donepezil.

Highlights

Research hot topics in the drug field are to design drug preparations with high-efficiency delivery [1,2,3]
To determine the drug loading and entrapment efficiency of drugloaded NPs, we established a standard curve for donepezil
The standard curve was drawn with the concentration of donepezil standard solution as the abscissa and absorbance value as the ordinate, with standard curve equation Y = −0 00373 + 0 01574X

Summary

Introduction

Research hot topics in the drug field are to design drug preparations with high-efficiency delivery [1,2,3]. Fat-soluble drugs more cross the blood–brain barrier for a pharmacological effect [6]. In preparing conventional formulations for craniocerebral diseases, increasing the drug solubility often requires a number of drug additions, which results in toxicity. The emergence of nanoformulations for injection has brought hope to solving the problem of drug delivery of fat-soluble drugs. Nanoparticles (NPs) represent a micropectin system composed of nanospheres or nanocapsules with particle size typically

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