Polypeptide and glycosaminoglycan polysaccharide as stabilizing polymers in nanocrystals for a safe ocular hypotensive effect.

Autor: Donia M; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, African organization unity street, P.O. Box 11566, Cairo, Egypt. Electronic address: marwadonia@pharma.asu.edu.eg., Osman R; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, African organization unity street, P.O. Box 11566, Cairo, Egypt., Awad GAS; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, African organization unity street, P.O. Box 11566, Cairo, Egypt., Mortada N; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, African organization unity street, P.O. Box 11566, Cairo, Egypt.
Jazyk: angličtina
Zdroj: International journal of biological macromolecules [Int J Biol Macromol] 2020 Nov 01; Vol. 162, pp. 1699-1710. Date of Electronic Publication: 2020 Aug 08.
DOI: 10.1016/j.ijbiomac.2020.07.306
Abstrakt: Improved ocular delivery of a poorly soluble anti-glaucoma drug, acetazolamide (ACZ), in a stable nanosuspension (NS) was the main target of the study. The anionic polypeptide, poly-γ-glutamic acid (PG) and the glycosaminoglycan, hyaluronic acid, were used to stabilize ACZ-NS prepared using the antisolvent precipitation (AS-PT) coupled with sonication technique. To endue in site biocompatibility with high tolerability, soya lecithin (SL) phospholipid has been also combined with polyvinyl alcohol (PVA). NS with uniform PS in the range 100-300 nm, high ζ > ±20 mV, and enhanced saturation solubility were produced. Targeting solvent removal with control on future particle growth, post-production processing of NS was done using spray drying. The carriers' composition and amount relative to ACZ-NS were optimized to allow for the production of a redispersible dry crystalline powder. Particles crystallinity was confirmed using X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) in liquid and spray dried NS. The modified Draize test proved the safety and tolerability following application to rabbit eyes accompanying an efficient ocular hypotensive activity using a steroid glaucoma model.
(Copyright © 2020 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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