Yun, Taehan and Lee, Sumin and Yun, Seowan and Cho, Daeyeong and Bang, Kyuho and Kim, Kyeongsoo (2024) Investigation of Stabilized Amorphous Solid Dispersions to Improve Oral Olaparib Absorption. Pharmaceutics, 16 (7). p. 958. ISSN 1999-4923
![[thumbnail of pharmaceutics-16-00958.pdf]](http://asian.go4publish.com/style/images/fileicons/text.png)
pharmaceutics-16-00958.pdf - Published Version
Download (5MB)
Abstract
In this study, we investigated the formulation of stable solid dispersions to enhance the bioavailability of olaparib (OLA), a therapeutic agent for ovarian cancer and breast cancer characterized as a BCS class IV drug with low solubility and low permeability. Various polymers were screened based on solubility tests, and OLA-loaded solid dispersions were prepared using spray drying. The physicochemical properties of these dispersions were investigated via scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier Transform Infrared Spectroscopy (FT-IR). Subsequent dissolution tests, along with assessments of morphological and crystallinity changes in aqueous solutions, led to the selection of a hypromellose (HPMC)-based OLA solid dispersion as the optimal formulation. HPMC was effective at maintaining the supersaturation of OLA in aqueous solutions and exhibited a stable amorphous state without recrystallization. In an in vivo study, this HPMC-based OLA solid dispersion significantly enhanced bioavailability, increasing AUC0–24 by 4.19-fold and Cmax by more than 10.68-fold compared to OLA drug powder (crystalline OLA). Our results highlight the effectiveness of HPMC-based solid dispersions in enhancing the oral bioavailability of OLA and suggest that they could be an effective tool for the development of oral drug formulations.
Item Type: | Article |
---|---|
Subjects: | Oalibrary Press > Medical Science |
Depositing User: | Managing Editor |
Date Deposited: | 20 Jul 2024 10:42 |
Last Modified: | 20 Jul 2024 10:42 |
URI: | http://asian.go4publish.com/id/eprint/3881 |