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Gliclazide-loaded Solid Lipid Nanoparticles: Development, Physicochemical characterization and in-situ single-pass intestinal permeability evaluation
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Ziba Islambulchilar   , Parvin Zakeri-Milani , Hadi Valizadeh , Akbar Saei |
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Abstract: (314 Views) |
Introduction: Gliclazide, a sulfonylurea specifically used for the treatment of non-insulin-dependent diabetes mellitus, exhibits low oral bioavailability due to its poor aqueous solubility and first pass metabolism. The aim of the present study is to develop, prepare and evaluate the physicochemical characteristics of gliclazide loaded solid lipid nanoparticles (SLN) and to determine and to compare the intestinal permeability of gliclazide loaded SLNs and free gliclazide using the single pass intestinal perfusion (SPIP) method in rat.
Methods and Materials: Solid lipid nanoparticles (SLN) were designed and prepared using different proportions of formulation components. Physicochemical characteristics of formulations including droplet size, poly dispersity index and zeta potential, encapsulation efficiency, drug loading and drug release were evaluated. SPIP technique was applied to determine intestinal permeability. Both free gliclazide and gliclazide loaded nanoparticles were perfused through a cannulated segment of rat jejunum. Outlet perfusates were collected every 10 min to 90 min and were analyzed by HPLC. Permeability coefficients (Peff) were calculated and compared.
Results: The optimized SLN formulation consists of 300 mg stearyl alcohol, 330 mg Brij 58 and 70 mg Transcutol P. Droplet size and PDI of optimized formulation were 81 nm and 0.13 respectively. The encapsulation efficiency of optimized SLN was 87.5 % and it has released more than 90 % of its drug content during 20 hours. The effective intestinal permeability of free gliclazide and gliclazide loaded SLNs were 1.34 × 10 -4 and 2.78 × 10-4 cm/s. Therefore loading in solid lipid nanoparticles led to a significant increase in intestinal permeability of gliclazide.
Conclusion: Solid lipid nanoparticles could be considered as promising tools for oral delivery of gliclazide according to appropriate physicochemical properties and observed increase in its intestinal permeability which could consequently enhance its oral bioavailability.
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| Keywords: Gliclazide, Solid lipid nanoparticle, Permeability, SPIP |
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Full-Text [PDF 263 kb]
(56 Downloads)
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Type of Study: Research |
Subject:
General
Received: 2023/09/16 | Accepted: 2023/08/23 | Published: 2023/08/23
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