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

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 drugloaded 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.

Characterization and evaluation of porous hydroxyapatite synthesized by oil-in-water method as carrier of donepezil for the preventive of Alzheimer’s disease by controlled release

“…Most drugs for AD treatment, including DPZ, are designed to be highly hydrophobic because the target region of these drugs is usually inside the brain; therefore, these drugs are designed to pass through the blood-brain barrier (BBB). Only hydrophobic and small molecule drugs can go through the BBB by blood circulation system [37,38]. DPZ is the leading compound for the treatment of AD in more than 50 countries.…”

Folate-Conjugated Chitosan-Pluronic P123 Nanogels: Synthesis and Characterizations towards Dual Drug Delivery

“…An increasing amount of the grafted P123 or a high content of P123 in the CP copolymer contributed to enlarging the CMC value. Many previous studies have also shown that conjugation with polysaccharides leads to a reduction of the CMC value of pluronics [6,32]. Chitosan attacks pluronic chains and shields the hydrophobic blocks from interaction with water reducing the interfacial free energy of the polymer-water system.…”

“…), fluorescent probes (pyrazole, etc. ), or genes/proteins can be protected by the hydrophilic segments organizing into the shell, whereas the pharmacokinetics of this compound become more significant [3][4][5][6][7]. Along with the advantage of a core-shell nanostructure, the introduction of natural polymers such as chitosan, heparin, or hyaluronic acid also helps to protect nanoparticles from opsonization due to the imparting of a stealth effect on the shell [8][9][10].…”

Synthesis of biopolymeric particles loaded with phosphorus and potassium: characterisation and release tests

“…The higher particle size of the alginate NPs negatively affects the rate of release of P and K; because with high particle size, the specific surface area of the NPs is reduced, and, therefore, the solubility and dissolution rate can be decreased [33]. a Data correspond to the carbonisation of alginate.…”