Development of Poly (Methyl vinyl ether-alt-maleic acid) Microneedles for Transdermal Delivery of Atorvastatin Calcium
Autor: | Pablo Serrano Castañeda, Eva M M Trinidad, José Juan Escobar-Chávez, Miriam Lopez Cervantes, Isabel Marlen Rodríguez Cruz, Luz María Melgoza Contreras, Clara L Domínguez Delgado |
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Rok vydání: | 2019 |
Předmět: |
Drug
Materials science Maleic acid Atorvastatin media_common.quotation_subject Skin Absorption Pharmaceutical Science 02 engineering and technology Biodegradable Plastics In Vitro Techniques Administration Cutaneous 030226 pharmacology & pharmacy 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Differential scanning calorimetry Drug Delivery Systems medicine Stratum corneum Animals Humans Transdermal media_common Skin chemistry.chemical_classification Drug Carriers Anticholesteremic Agents Maleates Polymer 021001 nanoscience & nanotechnology Biodegradable polymer Drug Liberation medicine.anatomical_structure chemistry Needles Polyethylenes 0210 nano-technology Biotechnology medicine.drug Biomedical engineering |
Zdroj: | Current pharmaceutical biotechnology. 21(9) |
ISSN: | 1873-4316 |
Popis: | Aims: Biodegradable polymeric microneedles containing atorvastatin calcium were developed in order to improve the percutaneous absorption of the drug, useful for the treatment of hypercholesterolemia. Background: The use of physical enhancers like microneedles have shown good results to increase the delivery of drugs through the skin, the use of microneedles has very important advantages for transdermal drug delivery, for example, they are painless, easy to use and safe, they increase time interval of drug activity, dose, and reductions in adverse reactions, they also offer, the facility to remove the system instantly of the skin. Objective: Develop polymer microneedles loaded with a calcium atorvastatin and evaluate them by Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), bioadhesion, postwetting- bioadhesion, breaking strength, drug release test and in vitro percutaneous absorption studies to demonstrate the use of microneedles atorvastatin is able to cross the skin. Methods: The microneedles were made with poly (methyl vinyl ether-alt-maleic acid) as biodegradable polymer using the technique of casting in solution in a mold. After solidification these microneedles were characterized by Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), bioadhesion, post-wetting-bioadhesion, breaking strength, drug release test and in vitro percutaneous absorption studies. Results: In general, the performances were satisfactory for optimal formulation in terms of DSC with no interactions between drug and excipients, SEM shows microneedles with a conical shape, bioadhesion of 1570 g.f, post wetting-bioadhesion of 1503.4 g.f, breaking strength of 1566.7g.f that is sufficient to disrupt Stratum corneum, good drug release and a flux of 33.4 μg/cm2*h with a tLag of 15.14 h for the in vitro percutaneous absorption. Conclusion: The results indicate that it is possible to generate microneedles to increase the percutaneous absorption of calcium atorvastatin transdermally, with the potential to be used as an alternative to the oral route for the treatment of dyslipidemias. |
Databáze: | OpenAIRE |
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