Anionic versus cationic bilosomes as oral nanocarriers for enhanced delivery of the hydrophilic drug risedronate.

Autor: Elnaggar YSR; Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt; Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Pharos University in Alexandria, Alexandria, Egypt. Electronic address: yosra.s.elnaggar@gmail.com., Omran S; Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt., Hazzah HA; Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Pharos University in Alexandria, Alexandria, Egypt., Abdallah OY; Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.
Jazyk: angličtina
Zdroj: International journal of pharmaceutics [Int J Pharm] 2019 Jun 10; Vol. 564, pp. 410-425. Date of Electronic Publication: 2019 Apr 25.
DOI: 10.1016/j.ijpharm.2019.04.069
Abstrakt: Albeit its well known potency as a postmenopausal osteoporosis treatment, Risedronate suffers from poor oral bioavailability and high oral toxicity. This is the first work to assess the potential of bilosomes to address challenges of RS oral delivery. Furthermore, impact of integrating cationic moiety into bilosomes on intestinal digestability and toxicity of RS nanovesicles was first investigated in this article. Prepared formulations were optimized based on physicochemical properties, digestibility, intestinal permeation and local toxicity studies. Optimized preparations were prepared by reversed phase evaporation technique with three extrusion cycles and loaded by 10 mg/ml RS. Molar lipid to bile salt to cholesterol ratio was adjusted to 4:1:1 at pH 5. Addition of cholesterol had significantly improved bilosomes stability to digestive media. Results also revealed that permeation of anionic vesicles increased permeation by 1.5 times more than RS solution and reduced drug toxicity by 2 folds. On the other hand, Cationic bilosomes showed good stability in GIT fluids but their induced oral toxicity could limit their use. In conclusion, bilosomes are superior over liposomes regarding protection of delivery system from the damaging effect of external in digestive bile salts. In addition, it decreases toxicity issues of orally administered drugs.
(Copyright © 2019 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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