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Mini-Tablets versus Nanoparticles for Controlling the Release of Amoxicillin: In vitro/In vivo Study.
- Source :
-
Drug design, development and therapy [Drug Des Devel Ther] 2020 Dec 07; Vol. 14, pp. 5405-5418. Date of Electronic Publication: 2020 Dec 07 (Print Publication: 2020). - Publication Year :
- 2020
-
Abstract
- Introduction: Controlling the drug release from the dosage form at a definite rate is the main challenge for a successful oral controlled-release drug delivery system. In this study, mini-tablets (MTs) and lipid/polymer nanoparticles (LPNs) of lipid polymer and chitosan in different ratios were designed to encapsulate and control the release time of Amoxicillin (AMX).<br />Methods: Physical characteristics and in vitro release profiles of both MT and LPN formulations were studied. Antimicrobial activity and oral pharmacokinetics of the optimum MT and LPN formulations in comparison to market tablet were studied in rats.<br />Results: All designed formulations of AMX as MTs and LPNs showed accepted characteristics. MT-6 (Compritol/Chitosan 1:1) showed the greatest retardation among all prepared minitablet preparations, releasing about 79.5% of AMX over 8 h. In contrast, LPN-11 (AMX: Cr 1:3/Chitosan 1 mg/mL) had the slowest drug release, revealing the sustained release of 80.9% within 8 h. The MIC of both optimized tablet formula (MT-6) and LPNs formula (LPN-11) was around two-fold lower than the control against H. pylori . The C <subscript>max</subscript> of MT-6 and LPN11 were non significantly different compared with the marketed AMX product. While the bioavailability experiment proved that the relative bioavailability of the AMX was 1.85 and 1.8 after the oral use of LPN11 and MT-6, respectively, compared to the market tablet.<br />Conclusion: The results verified that both controlled-release mini-tablets and lipid/polymer nanoparticles can be used for sustaining the release and hence improve the bioavailability of amoxicillin.<br />Competing Interests: The authors report no conflicts of interest in this work.<br /> (© 2020 Gaber et al.)
- Subjects :
- Amoxicillin chemistry
Amoxicillin metabolism
Animals
Anti-Bacterial Agents chemistry
Anti-Bacterial Agents metabolism
Biological Availability
Drug Liberation
Kinetics
Male
Microbial Sensitivity Tests
Nanoparticles metabolism
Rats
Rats, Wistar
Tablets
Amoxicillin pharmacology
Anti-Bacterial Agents pharmacology
Helicobacter pylori drug effects
Nanoparticles chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1177-8881
- Volume :
- 14
- Database :
- MEDLINE
- Journal :
- Drug design, development and therapy
- Publication Type :
- Academic Journal
- Accession number :
- 33324038
- Full Text :
- https://doi.org/10.2147/DDDT.S285522