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. 2012:7:4787-96.
doi: 10.2147/IJN.S34312. Epub 2012 Sep 4.

Dual drug delivery system for targeting H. pylori in the stomach: preparation and in vitro characterization of amoxicillin-loaded Carbopol® nanospheres

Sree Harsha  1
Affiliations

Dual drug delivery system for targeting H. pylori in the stomach: preparation and in vitro characterization of amoxicillin-loaded Carbopol® nanospheres

Sree Harsha. Int J Nanomedicine. 2012.

Abstract

Background and methods: A dual (immediate/sustained-release) oral amoxicillin suspension was developed as a new dosage form to eradicate Helicobacter pylori. Carbopol®-loaded amoxicillin nanospheres could bind with the mucosa after delivery to the stomach and could increase the efficiency of the drug, providing both an immediate and a sustained action.

Results: The objective of this research was to develop amoxicillin nanospheres using a spray-drying technique and to investigate such features as their particle size, drug content, percentage yield, surface morphology, in vitro release, and stability. The nanospheres had a particle size range of 280-320 nm after optimizing the preparation method using a central composite design. The drug content and percentage yield was 85.3% ± 0.7% and 92.8% ± 0.9%, respectively. The in vitro release profile of the amoxicillin nanospheres was consistent with a Korsmeyer-Peppas pattern, and the release after one hour was 19%, while for the original drug, amoxicillin, under the same conditions, 90% was released in the first 30 minutes.

Conclusion: The nanospheres used in this study enabled controlled release of amoxicillin over an extended period of time for up to 12 hours and the formulation was stable for 12 months.

Keywords: Helicobacter pylori; amoxicillin; nano spraydryer; nanospheres; optimization.

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Figures

Figure 1
Figure 1
Scanning electron micrograph of spraydried nanospheres.
Figure 2
Figure 2
Three-dimensional plot showing the effect of inlet temperature and Carbopol concentration, and their mutual interaction on particle size.
Figure 3
Figure 3
Three-dimensional plot showing the effect of feed flow rate and inlet temperature, and their mutual interaction on particle size.
Figure 4
Figure 4
Three-dimensional plot showing the effect of Carbopol concentration and feed flow rate, and their mutual interaction on particle size.
Figure 5
Figure 5
Particle size distribution for amoxicillin nanospheres.
Figure 6
Figure 6
In vitro drug release from amoxicillin alone and from amoxicillin nanospheres.
Figure 7
Figure 7
In vitro release profile for amoxicillin nanospheres (Kosmeyer-Peppas release pattern).
Figure 8
Figure 8
Drug content plot for amoxicillin nanospheres in real-time storage conditions.
See this image and copyright information in PMC

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