Peyer'e patch targeting of Isradipine loaded Solid Lipid Nanoparticles: It's cellular uptake study

Autor: Hitesh Katariya, Jagruti B. Prajapati, Ravish J. Patel
Rok vydání: 2018
Předmět:
Zdroj: Journal of Drug Delivery Science and Technology. 43:318-326
ISSN: 1773-2247
DOI: 10.1016/j.jddst.2017.10.017
Popis: Isradipine (ISR), BCS Class II antihypertensive drug undergoes extensive first pass metabolism (FPM) with low bioavailability (15–24%). FPM may be avoided by formulating ISR loaded Solid Lipid Nanoparticles (SLN). Lipidic ISR-SLN get absorbed through M-Cells of peyer's patches. Preformulation study was performed. Dynasan 114 was selected as lipid. Poloxamer 407 was selected as surfactant. ISR-SLN was prepared using High Speed Homogenization-Ultrasonication method, optimized by 32 full factorial design. ISR-SLN was lyophilized. (1:5 = solid: cryoprotactant). Process parameters like homogenization speed, time and sonication cycle were also optimized. In-Vitro % Cummulative drug release(%CDR) study of ISR-SLN (dispersion & lyophilized) was performed using dialysis bag method in 0.1 N HCl+2% tween 80 for 2 h (obtained 10% drug release) than in phosphate buffer Ph 7.4 + 2% tween 80 (Aprx. 100% drug release after 130hrs, followed higuchi model). Ex-Vivo %CDR was performed using chicken duodenum in same condition as In-Vitro. Characterization was done using zeta potential (−21.5 mv), TEM(Spherical shape and smooth surface), MPS(204 nm), %EE (90.85 ± 3.55%), XRD, DSC, FT-IR. Confocal Laser Scanning Microscopy of Rodamine B labeled ISR-SLN was performed to study uptake of ISR-SLN through M-Cells, Peyer's Patches. Stability study of 45 days shows the ISR-SLN is stable. ISR-SLN give controlled release, permeates M-Cell of Peyer's patch and are stable.
Databáze: OpenAIRE
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