Enlarged Pore Size Chiral Mesoporous Silica Nanoparticles Loaded Poorly Water-Soluble Drug Perform Superior Delivery Effect.

Yingyu Guo,Kaijun Gou,Xueyu Pu,Yumei Wang,Sanming Li,Baixue Yang,Heran Li

doi:10.3390/molecules24193552

Yingyu Guo, Kaijun Gou + Show 5 more

Open Access

https://doi.org/10.3390/molecules24193552

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Abstract

Large mesopores of chiral silica nanoparticles applied as drug carrier are worth studying. In this study, chiral mesoporous silica nanoparticles (CMSN) and enlarged chiral mesoporous silica nanoparticles (E-CMSN) with a particle size from 200 to 300 nm were synthesized. Fourier transform infrared spectrometer (FTIR), circular dichroism spectrum, scanning electron microscopy (SEM), transmission electron microscope (TEM), and nitrogen adsorption/desorption measurement were adopted to explore their characteristics. The results showed that the surface area, pore volume, and pore diameter of E-CMSN were higher than those of CMSN due to enlarged mesopores. Poorly water-soluble drug nimesulide (NMS) was taken as the model drug and loaded into carriers using adsorption method. After NMS was loaded into CMSN and E-CMSN, most crystalline NMS converted to amorphous phase and E-CMSN was superior. The anti-inflammatory pharmacodynamics and in vivo pharmacokinetics results were consistent with the wetting property and in vitro drug dissolution results, verifying that NMS/E-CMSN exhibited superior NMS delivery system based on its higher oral relative bioavailability and anti-inflammatory effect because its enlarge mesopores contributed to load and release more amorphous NMS. The minor variations in the synthesis process contributed to optimize the chiral nano-silica drug delivery system.

Highlights

In recent years, mesoporous silica nanoparticles (MSN) fabricated based on various kinds of templates have aroused a lot of interest owing to their rigid frame, good biocompatibility and biodegradability, unique structural features, and facile surface modification [1,2,3,4]
N-H deformation vibration at 1635.2 cm−1 and carbonyl stretching band at 1699.2 cm−1 that shown in spectrum of chiral mesoporous silica nanoparticles (CMSN) originated from the chiral groups that grafted onto the silica frame [7]
The two peaks were seen with a little lower shift than CMSN (N-H deformation vibration at 1632.4 cm−1 and carbonyl stretching band at 1698.7 cm−1 from the spectrum of enlarged chiral mesoporous silica nanoparticles (E-CMSN)), implying that the existence state of functional groups in E-CMSN can slightly different from CMSN for the pore enlargement management

Summary

Introduction

Mesoporous silica nanoparticles (MSN) fabricated based on various kinds of templates have aroused a lot of interest owing to their rigid frame, good biocompatibility and biodegradability, unique structural features (tunable mesopores in the range of 2–50 nm, large pore volume as well as total surface area), and facile surface modification [1,2,3,4]. Enlarging the mesopores of CMSN can load biomacromolecule and protect its activity [9]. It was reported that mesopores in the range of 3.8 to 20 nm can be regulated by controlling systemic pH. The pH cannot be precisely controlled in the sol to gel preparing process, and the mesoporous range was Molecules 2019, 24, 3552; doi:10.3390/molecules24193552 www.mdpi.com/journal/molecules

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