Drug Design, Development and Therapy (Dec 2020)
Mini-Tablets versus Nanoparticles for Controlling the Release of Amoxicillin: In vitro/In vivo Study
Abstract
Dalia A Gaber,1,2 Hessah S Alhawas,3 Fatimah A Alfadhel,3 Siham A Abdoun,1,4 Amal M Alsubaiyel,1 Rehab M Alsawi5 1Department of Pharmaceutics, College of Pharmacy, Qassim University, Buraidah, kingdom of saudi arabia; 2Department of Quality Control & Quality Assurance, Holding Company for Biological Products and Vaccines, Cairo, Egypt; 3College of Pharmacy, Qassim University, Buraidah, kingdom of saudi arabia; 4National Medicine Quality Control Laboratory, National Medicine and Poisons Board, Sudan; 5King Faisal Specialist Hospital and Research Center, Riyadh, kingdom of saudi arabiaCorrespondence: Dalia A Gaber Department of PharmaceuticsCollege of pharmacy, Qassim university, Buridah, Saudi arabiaTel +20 1001523222Email [email protected]: 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).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.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 Cmax 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.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.Keywords: lipid-polymer, nanoparticles, amoxicillin, bioavailability, mini-tablet, chitosan, sustain release
