Abstract

The aim of this study was to evaluate the characterized hydration method to prepare nanoparticles using Soluplus, a block copolymer with amphipathic properties, and distearoyl phosphatidyl ethanolamine (DSPE)-PEG2000 owing to particle size distribution, zeta potential, particle stability, and transmission electron microscopy (TEM) observed and 31P-NMR spectra. The results showed that, in a suspension of DSPE-PEG2000 and Soluplus at a ratio of 1/1, the prepared microparticles were stable for five days in the dark and at 25 °C. It was also confirmed that the 1/1 suspension of DSPE-PEG2000/Soluplus was stable for five days under the same conditions with the magnesium chloride solution. TEM measurements confirmed the presence of micelle-like particles of 50 to 150 nm in the 1/1 ratio mix of DSPE-PEG2000/Soluplus. 31P-NMR spectral data confirmed that DPSE-PEG2000/Soluplus at mixing ratio of 1/1 has a strong intermolecular with the phosphate group, indicated by the fact that the peak shift and the full width at half maximum were the largest compared with DSPE-PEG2000 with the intermolecular interaction. On the basis of the findings of this study, we conclude that microparticles can be formed using DSPE-PEG2000 and Soluplus via the hydration method, and that the optimum weight ratio of DSPE-PEG2000 to Soluplus is 1/1.

Highlights

  • Nanocarriers are reported to have several benefits in pharmacology, including improved solubility and stability of poorly water-soluble compounds [1], improved pharmacokinetics and biodistribution [2], and delivery to specific sites, allowing for better control of the release of drugs and reduced side effects [3,4]

  • Nanocarriers are used as a base for many drug delivery system (DDS) preparations and include polymeric micelles, liposomes, and so on [8,9]

  • Polymeric micelles have the advantages of low critical micelle concentration, narrow particle size distribution, and low dissociation rate [12], as well as high drug filling amount [13,14]

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Summary

Introduction

Nanocarriers are reported to have several benefits in pharmacology, including improved solubility and stability of poorly water-soluble compounds [1], improved pharmacokinetics and biodistribution [2], and delivery to specific sites, allowing for better control of the release of drugs and reduced side effects [3,4]. It is possible to change the application by changing the physiochemical properties of nanocarriers, including composition, shape, surface charge, functional group, and surface properties such as PEGylation [5]. The micelle has a hydrophilic structure on the outer shell and a hydrophobic structure on the inner side, which together form a nano-size that protects the poorly water-soluble drug with its own outer shell and disperses the poorly water-soluble compound in water. This allows for the dissolution of poorly water-soluble compounds in an aqueous medium [10,11]. Polymeric micelles have the advantages of low critical micelle concentration, narrow particle size distribution, and low dissociation rate [12], as well as high drug filling amount [13,14]

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