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access icon free Production of a new platform based on fumed and mesoporous silica nanoparticles for enhanced solubility and oral bioavailability of raloxifene HCl

© The Institution of Engineering and Technology
Received 07/08/2018, Accepted 15/01/2019, Revised 04/10/2018, Published 28/01/2019

The purpose of the present study was to compare mesoporous and fumed silica nanoparticles (NPs) to enhance the aqueous solubility and oral bioavailability of raloxifene hydrochloride (RH). Mesoporous silica NPs (MSNs) and fumed silica NPs were used by freeze-drying or spray-drying methods. MSNs were obtained with different ratios of cetyltrimethylammonium bromide. Saturation solubility of the NPs was compared with the pure drug. The optimised formulation was characterised by scanning electron microscopy (SEM), X-ray diffraction (XRD) and differential scanning calorimetry. The pharmacokinetic studies were done by oral administration of a single dose of 15 mg/kg of pure drug or fumed silica NPs of RH in Wistar rats. MSNs enhanced the solubility of RH from 19.88 ± 0.12 to 76.5 μg/ml. Freeze-dried fumed silica increased the solubility of the drug more than MSNs (140.17 ± 0.45 μg/ml). However, the spray-dried fumed silica caused about 26-fold enhancement in its solubility (525.7 ± 93.5 μg/ml). Increasing the ratio of silica NPs enhanced the drug solubility. The results of XRD and SEM analyses displayed RH were in the amorphous state in the NPs. Oral bioavailability of NPs showed 3.5-fold increase compared to the pure drug. The RH loaded fumed silica NPs prepared by spray-drying technique could more enhance the solubility and oral bioavailability of RH.

Inspec keywords: scanning electron microscopy; solubility; freezing; mesoporous materials; nanomedicine; X-ray diffraction; biochemistry; differential scanning calorimetry; spraying; amorphous state; biomedical materials; drug delivery systems; nanofabrication; silicon compounds; drying; drugs; nanoparticles

Other keywords: aqueous solubility; fumed silica nanoparticles; spray-dried; differential scanning calorimetry; mesoporous silica NPs; freeze-drying; spray-drying technique; drug solubility; fumed silica NPs; freeze-dried fumed silica; mesoporous silica nanoparticles; saturation solubility; oral administration

Subjects: Methods of nanofabrication and processing; Biomedical materials; Structure of solid clusters, nanoparticles, nanotubes and nanostructured materials; Nanotechnology applications in biomedicine; Patient care and treatment

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