Formulation of Chitosan-Coated Piperine NLCs: Optimization, In Vitro Characterization, and In Vivo Preclinical Assessment
| Autor: | Mohd Yasir, Mohammed Elmowafy, Syed Sarim Imam, Nabil K. Alruwaili, Khalid Saad Alharbi, Elshaer F Mohammed, Ziad H. Al-Oanzi, Omar Awad Alsaidan, Ameeduzzafar Zafar |
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| Rok vydání: | 2021 |
| Předmět: |
Polyunsaturated Alkamides
Pharmaceutical Science Administration Oral Absorption (skin) Aquatic Science Chitosan chemistry.chemical_compound Alkaloids Piperidines In vivo Drug Discovery medicine Animals Benzodioxoles Particle Size Ecology Evolution Behavior and Systematics Drug Carriers Chromatography Ecology General Medicine Permeation Streptozotocin Lipids In vitro Nanostructures Rats chemistry Piperine Particle size Agronomy and Crop Science medicine.drug |
| Zdroj: | AAPS PharmSciTech. 22(7) |
| ISSN: | 1530-9932 |
| Popis: | In the present research work, surface-modified nanostructured lipid carriers (NLCs) with chitosan (CH) were prepared to improve the therapeutic efficacy of piperine (PP). NLCs were developed and optimized (CH-PP-NLCs-opt) by design expert software and the selected NLCs surface was coated with chitosan (0.2% w/v). CH-PP-NLCs-opt have shown a particle size of 149.34 ± 4.54 nm and entrapment efficiency of 80.65 ± 1.23%. The results of the solid-state characterization study exhibited that PP enclosed in lipids and present amorphous form. It might be due to the nanoparticle size of NLCs. The drug release study revealed PP-NLCs-opt and CH-PP-NLCs-opt exhibited significant (P < 0.05) difference in PP release (88.87 ± 5.23% and 76.34 ± 4.54%) as compared to pure PP (19.02 ± 2.87%). CH-PP-NLCs-opt exhibited strong bioadhesion than PP-NLCs-opt which has a positive influence the drug permeation and absorption. CH-PP-NLCs-opt showed higher permeation (1083.34 ± 34.15 μg/ cm2) than pure PP (106.65 ± 15.44 μg/cm2) and PP-NLCs-opt (732.45 ± 28.56 μg/ cm2). The significantly enhanced bioavailability of PP was observed from CH-PP-NLCs-opt (3.76- and 1.21-fold) than PP-dispersion and PP-NLCs-opt. The diabetes was induced in rats by a single intraperitoneal administration of streptozotocin (STZ, 40 mg/kg, citrate buffer pH 4.5), and results revealed that PP-NLCs-opt and CH-PP-NLCs-opt reduce the blood glucose level (28.26% and 36.52% respectively) as compared to PP-dispersion (10.87%). It also helps to maintain the altered biochemical parameters. In conclusion, CH-PP-NLC can be a novel oral nanocarrier for the management of diabetes. |
| Databáze: | OpenAIRE |
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