Chitosan-TPP nanoparticles stabilized by poloxamer for controlling the release and enhancing the bioavailability of doxazosin mesylate: in vitro, and in vivo evaluation

Autor:	Khaled M. Hosny, Bader M Aljaeid, Khalid M. El-Say
Rok vydání:	2019
Předmět:	Pharmacology Mesylate Organic Chemistry Pharmaceutical Science 02 engineering and technology Poloxamer 021001 nanoscience & nanotechnology 030226 pharmacology & pharmacy Doxazosin Mesylate Bioavailability Chitosan 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine chemistry Pharmacokinetics In vivo Drug Discovery 0210 nano-technology Homogenization (biology)
Zdroj:	Drug Development and Industrial Pharmacy. 45:1130-1139
ISSN:	1520-5762 0363-9045
DOI:	10.1080/03639045.2019.1597105
Popis:	Objective: Control the release and enhance the bioavailability of chitosan-doxazosin mesylate nanoparticles (DM-NPs). Significance: Improve DM bioavailability for the treatment of benign prostatic hyperplasia and hypertension. Methods: Plackett-Burman design was utilized to screen the variables affecting the quality of DM-NPs prepared by ionic gelation method. The investigated variables were initial drug load (X1), chitosan percentage (X2), tripolyphosphate sodium (TPP) percentage (X3), poloxamer percentage (X4), homogenization speed (X5), homogenization time (X6) and TPP addition rate (X7). The prepared DM-loaded NPs have been fully evaluated for particle size (Y1), Zeta potential (Y2), production yield (Y3), entrapment efficiency (Y4), loading capacity (Y5), initial burst (Y6), and cumulative drug release (Y7). Finally, DM pharmacokinetic has been investigated on healthy albino male rabbits by means of non-compartmental analysis. Results: The combination of variables showed variability of Y1, Y2, and Y3 equal to 122-710 nm, 3.49-23.63 mV, and 47.31-92.96%, respectively. While Y4 and Y5, reached 99.87%, and 8.53%, respectively. The prepared NPs revealed that X2, X3, and X4 are the variables that play the important role in controlling the release behavior of DM from the NPs. The in vivo pharmacokinetic results indicated the enhancement in bioavailability of DM by 7 folds compared to drug suspension and the mean residence time prolonged to 23.72 h compared to 4.7 h of drug suspension. Conclusion: The study proved that controlling the release of DM from NPs enhance its bioavailability and improve the compliance of patients with hypertension or benign prostatic hyperplasia.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::f397cba22405afca56c79fa56f27db5b https://doi.org/10.1080/03639045.2019.1597105 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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