Formulation development of a carrageenan based delivery system for buccal drug delivery using ibuprofen as a model drug

Kianfar, Farnoosh, Antonijevic, Milan D., Chowdhry, Babur Z. and Boateng, Joshua S. (2011) Formulation development of a carrageenan based delivery system for buccal drug delivery using ibuprofen as a model drug. Journal of Biomaterials and Nanobiotechnology, 2 (05A). pp. 582-595. ISSN 2158-7027 (print), 2158-7043 (online)

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Abstract

Solvent cast films are used as oral strips with potential to adhere to the mucosal surface, hydrate and deliver drugs
across the buccal membrane. The objective of this study was the formulation development of bioadhesive films with
optimum drug loading for buccal delivery. Films prepared from κ-carrageenan, poloxamer and polyethylene glycol or
glycerol, were loaded with ibuprofen as a model water insoluble drug. The films were characterized using texture
analysis (TA), hot stage microscopy (HSM), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA),
scanning electron microscopy (SEM), x-ray powder diffraction (XRPD), high performance liquid chromatography
(HPLC) and in vitro drug dissolution. Optimized films were obtained from aqueous gels containing 2.5% w/w κ-carrageenan
911, 4% w/w poloxamer 407 and polyethylene glycol (PEG) 600 [5.5% w/w (non-drug loaded) and 6.5% w/w
(drug loaded)]. A maximum of 0.8% w/w ibuprofen could be incorporated into the gels to obtain films with optimum
characteristics. Texture analysis confirmed that optimum film flexibility was achieved from 5.5% w/w and 6.5% (w/w)
of PEG 600 for blank films and ibuprofen loaded films respectively. TGA showed residual water content of the films as
approximately 5%. DSC revealed a Tg for ibuprofen at −53.87°C, a unified Tm for PEG 600/poloxamer mixture at
32.74°C and the existence of ibuprofen in amorphous form, and confirmed by XRPD. Drug dissolution at a pH simulating
that of saliva showed that amorphous ibuprofen was released from the films at a faster rate than the pure crystalline
drug. The results show successful design of a carrageenan and poloxamer based drug delivery system with potential for
buccal drug delivery and showed the conversion of crystalline ibuprofen to the amorphous form during film formation.

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