Nasal Mucoadhesive Microspheres of Lercanidipine with Improved Systemic Bioavailability and Antihypertensive Activity
| Autor: | Ameeduzzafar, Monica Thappa, Pradeep Kumar Singh, Bhupinder Singh, Sunil K. Panda, Sarwar Beg, Nabil K. Alruwaili, Khalid Saad Alharbi, Mahfoozur Rahman |
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| Rok vydání: | 2020 |
| Předmět: |
Drug
Chromatography Central composite design biology media_common.quotation_subject Lercanidipine Pharmaceutical Science 02 engineering and technology 021001 nanoscience & nanotechnology 030226 pharmacology & pharmacy Microsphere Bioavailability 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine chemistry Drug Discovery medicine biology.protein Glutaraldehyde Particle size Bovine serum albumin 0210 nano-technology media_common medicine.drug |
| Zdroj: | Journal of Pharmaceutical Innovation. 16:237-246 |
| ISSN: | 1939-8042 1872-5120 |
| Popis: | The current study entails the design, development, and optimization of nasal mucoadhesive microspheres of lercanidipine with improved systemic bioavailability for the management of hypertension. Mucoadhesive microspheres of lercanidipine were prepared by solvent evaporation and polymerization method using bovine serum albumin (BSA) as the carrier and glutaraldehyde as the chelating agent. For screening the material and process variables, Taguchi design revealed the major influence of BSA concentration and glutaraldehyde volume as the critical factors for the preparation of microspheres. These factors were systematically optimized using Central Composite design to evaluate the particle size, entrapment efficiency, and in vitro drug release from the microspheres as the response variables. The optimized microspheres were prepared using 4.4% BSA and 0.25-mL glutaraldehyde, and stirring speed at 1500 rpm, which exhibited particle size of 34 μm, entrapment efficiency of 88.6%, Q6h of 94.67%, T60% of 3.2 h, and bioadhesion efficiency of 93.2%. In vivo pharmacokinetics in rabbits showed remarkable superiority of the optimized nasal microspheres (p |
| Databáze: | OpenAIRE |
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