Investigating the Effects of Loading Factors on the In Vitro Pharmaceutical Performance of Mesoporous Materials as Drug Carriers for Ibuprofen.

Junmin Lai,Mingzhong Li,Peter Scholes,Wu Lin

doi:10.3390/ma10020150

Junmin Lai, Mingzhong Li + Show 2 more

Open Access

https://doi.org/10.3390/ma10020150

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Abstract

The aim of the study was to investigate the effects of the loading factors, i.e., the initial drug loading concentration and the ratio of the drug to carriers, on the in vitro pharmaceutical performance of drug-loaded mesoporous systems. Ibuprofen (IBU) was used as a model drug, and two non-ordered mesoporous materials of commercial silica Syloid® 244FP (S244FP) and Neusilin® US2 (NS2) were selected in the study. The IBU-loaded mesoporous samples were prepared by a solvent immersion method with a rotary evaporation drying technique and characterized by polarized light microscopy (PLM), Fourier transform infrared (FTIR) spectroscopy, X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC). Dissolution experiments were performed in simulated gastric media at 37 °C under non-sink conditions. The concentration of IBU in solution was determined by HPLC. The study showed that the dissolution rate of IBU can be improved significantly using the mesoporous S224FP carriers due to the conversion of crystalline IBU into the amorphous form. Both of the loading factors affected the IBU dissolution kinetics. Due to the molecular interaction between the IBU and NS2 carriers, the loading factors had little effects on the drug release kinetics with incomplete drug desorption recovery and insignificant dissolution enhancement. Care and extensive evaluation must therefore be taken when mesoporous materials are chosen as carrier delivery systems.

Highlights

Oral ingestion is the most common route of administration for drugs due to convenience and low cost
For the Syloid® 244FP (S244FP) carriers, there was no evidence of chemical interaction between the host and loaded IBU shown in the Fourier transform infrared (FTIR) results in Figure 2a; the loading factors played essential loaded IBU shown in the FTIR results in Figure 2a; the loading factors played essential roles roles in the drug physical state and release kinetics
The loading factors of the initial drug loading concentration and ratio of drug to carriers were studied for two different mesoporous carriers of S244FP and Neusilin® US2 (NS2)

Summary

Introduction

Oral ingestion is the most common route of administration for drugs due to convenience and low cost. A major challenge in designing oral dosage forms is poor bioavailability due to many factors, such as drug permeability, aqueous solubility and dissolution rate. Poor water solubility has currently been attributed to almost half of the new molecular entities (NMEs) synthesised annually by pharmaceutical companies [1]. Among many different technologies to improve the drug solubility/dissolution rate, such as solid dispersions, nanocrystals, soluble cyclodextrin complexes and self-emulsifying drug delivery systems [1], a delivery approach using mesoporous materials as drug carriers to improve poorly water-soluble active pharmaceutical ingredients (APIs) has shown high potential [2,3].

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