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Drug Dev Ind Pharm. 2014 Mar;40(3):361-9. doi: 10.3109/03639045.2012.762655. Epub 2013 Apr 19.

Development and physico-mechanical characterization of carrageenan and poloxamer-based lyophilized matrix as a potential buccal drug delivery system.

Drug development and industrial pharmacy

Farnoosh Kianfar, Isaac Ayensu, Joshua S Boateng

Affiliations

  1. Department of Pharmaceutical, Chemical and Environmental Sciences, School of Science, University of Greenwich , Chatham Maritime, Kent , UK.

PMID: 23600651 DOI: 10.3109/03639045.2012.762655

Abstract

CONTEXT AND OBJECTIVES: The buccal mucosa presents a unique surface for non-invasive drug delivery and also avoids first-pass metabolism. The objective of this study was the formulation development of polymeric mucoadhesive lyophilized wafers as a matrix for potential buccal drug delivery.

MATERIALS AND METHODS: Differential scanning calorimetry (DSC) was used to develop an optimum freeze-cycle, incorporating an annealing step. The wafers were prepared by lyophilization of gels containing three polymers, κ-carrageenan (CAR 911), poloxamer (P407) and polyethylene glycol 600 (PEG 600). The formulations were characterized using texture analysis (for mechanical and mucoadhesion properties), hydration studies, thermogravimetric analysis (TGA), DSC, X-ray powder diffraction (XRPD) and scanning electron microscopy (SEM).

RESULTS AND DISCUSSION: DSC showed the eutectic temperature (12.8 °C) of the system where the liquid solution and pure solids both existed at a fixed pressure which helped determine the freeze-annealing cycle at 55 °C for 7 h. Mechanical resistance to compression, hydration and mucoadhesion studies showed that optimized wafers were obtained from aqueous gels containing 2% w/w CAR 911, 4% w/w P407 and 4.4% w/w PEG 600. TGA showed residual water of approximately 1% and SEM showed a porous polymeric network that made ease of hydration possible.

CONCLUSIONS: Lyophilized wafers by freeze-drying gels containing 2% w/w CAR 911, 4% w/w P407 and 4.4% w/w PEG 600 with optimum physico-mechanical properties has been achieved.

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