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- Title
ETOPOSIDE AMORPHOUS SOLID DISPERSION FOR IMPROVED ORAL BIOAVAILABILITY: FORMULATION, CHARACTERIZATION, PHARMACOKINETIC AND CYTOTOXICITY STUDIES.
- Authors
Ghule, Prashant J.; Bairagi, Shripad M.; Gilhotra, Ritu M.
- Abstract
Etoposide is a well-known anti-tumor agent used to treat a variety of cancers. Although it is a BCS class IV drug, applications are restricted due to poor solubility and bioavailability. Hence, the current research was designed to overcome these pitfalls. A total of 16 formulation batches were developed using the physical mixture and kneading method and optimized by Design-Expert® software. A selected batch was evaluated using solubility, differential scanning calorimetry, X-ray diffraction, motic microscopy, scanning electron microscopy, Fourier transform infrared (FTIR), gastrointestinal distribution, pharmacokinetic and cytotoxicity study. The results showed that the saturated solubility of formulation was 19.76 mg mL-1. FTIR showed C-O=1646 cm-1, and C-H=2956 cm-1. The distribution study indicated 9.11, 5.39 and 4.23 µg mL-1 colon concentrations at 8h, 16h, and 24h, respectively. The Cmax and AUC were found at 741.17±12.29 ng mL-1 and 3089.23 ±34.69 ng mL-1 with less viability on HeLa cells. Therefore, the study investigates the developed solid dispersions enhanced solubility and bioavailability with an antiproliferative effect.
- Subjects
CYTOTOXINS; AMORPHOUS substances; DRUG solubility; ITRACONAZOLE; BIOAVAILABILITY; DISPERSION (Chemistry); PHARMACOKINETICS
- Publication
Indian Drugs, 2023, Vol 60, Issue 9, p57
- ISSN
0019-462X
- Publication type
Article
- DOI
10.53879/id.60.09.13786