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.
Highlights
The oral route is the most common means of administering pharmacological agents [1] because of advantages such as economy, convenience and patient compliance
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
The initial stages in the formulation of the films involved polymer swelling, hydration and subsequent formation of uniform and flowing gels for drying. κ-carrageenan 911 formed a firm gel which produced a flexible film in the presence of polyethylene glycol (PEG) 600 while the κ-carrageenan 812 gel was strong; the resulting film was very brittle even after the addition of plasticizer
Summary
The oral route is the most common means of administering pharmacological agents [1] because of advantages such as economy, convenience and patient compliance. Films have potential as buccal drug delivery systems owing to their ease of administration (currently used as fast dissolving oral strips) and ease of hydration on contact with mucosal surfaces to allow drug diffusion out of the swollen gel [5]. They are limited by low drug loading capacity because of their thin nature [6]. Not all film forming polymers are bioadhesive and improvements in bioadhesivity of such formulations
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