Pharmacokinetic evaluation of microgels for targeted and sustained delivery of acid labile active pharmaceutical agent in animal model
| Autor: | Nazar Mohammad Ranjha, Fareeha Rashid, Hina Raza, Zermina Rashid |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Drug
Chromatography media_common.quotation_subject Pharmaceutical Science 02 engineering and technology 021001 nanoscience & nanotechnology Methacrylate 030226 pharmacology & pharmacy Esomeprazole 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine chemistry Pharmacokinetics In vivo Drug delivery medicine Suspension polymerization Itaconic acid 0210 nano-technology media_common medicine.drug |
| Zdroj: | Journal of Drug Delivery Science and Technology. 57:101770 |
| ISSN: | 1773-2247 |
| Popis: | The study was aimed to evaluate the feasibility of chemically crosslinked pH responsive copolymeric microgels of 2-hydroxyethyl methacrylate and itaconic acid (p (HEMA-co-IA)) for targeted and sustained delivery of acid labile active pharmaceutical agents. Esomeprazole (model drug) was loaded by equilibrium swelling technique into microgels, obtained by suspension polymerization. The resultant microgels were spherical with average size of 6.43 ± 1.2 μm and percent esomeprazole loading was 65 ± 1.3%. In vitro dissolution studies confirmed the potential use of p (HEMA-co-IA) microgels to protect the drug from acidic pH of the stomach and to deliver the drug in response to intestinal pH over extended period of time. A single dose non-compartmental pharmacokinetic evaluation was performed in healthy rabbits in order to investigate the in vivo performance. The results showed delayed and extended release of the drug from the microgels, with decreased Cmax, prolonged tmax, increased AUC0-t and prolonged MRT in comparison to oral drug solution. The differences were statistically significant. The study concluded that p (HEMA-co-IA) microgels have potential for preferential drug delivery into higher pH environment over prolonged period of time. |
| Databáze: | OpenAIRE |
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