In situ composite ion-triggered gellan gum gel incorporating amino methacrylate copolymer microparticles: a therapeutic modality for buccal applicability

Abstract

The aim of the current investigation is to delineate the buccal applicability of an in situ composite gel containing aceclofenac (AC) amino methacrylate copolymer microparticles (MPs), surmounting limitations of oral existing conventional therapy. AC Eudragit RL100 MPs were fabricated and statistically optimized using 2²4¹ factorial design. Better buccal applicability and enhanced localization were achieved by combining the optimum MPs with in situ ion-activated gellan gum gel. The crosslinking and gelation of in situ gel were investigated by morphological and solid state characterizations. Suitability for buccal delivery and in vivo therapeutic efficacy in inflammation model of rats were also assessed. Results showed that the best performing formula displayed particle size (PS) of 51.00 µm and high entrapment efficiency (EE%) of 94.73%. MPs were successfully entrapped inside the gel network of the composite system. Gelation tendency, pH, shear-thinning properties and mucoadhesivity of the prepared in situ composite gel guaranteed its buccal suitability. Sustained AC release features and promising in vitro anti-arthritic response were also demonstrated. Moreover, consistent and prolonged in vivo anti-inflammatory effect was achieved, relative to standard AC. Taken together; this study proves the potential of in situ composite gel as an appropriate therapeutic proposal for AC buccal delivery.

Graphical Abstract

Keywords:

• Eudragit RL100
• microparticles
• gellan gum
• ion-triggered gel
• aceclofenac
• buccal delivery

Acknowledgements

The authors would like to acknowledge Evonik Pharma, GmbH, Darmstadt, Germany and E.I.P.I.C.O. Company, Cairo, Egypt for their kind supply of Eudragit RL100 and HPMC respectively. The authors would also like to thank Bristol-Myers Squibb Company, Cairo, Egypt for their kind supply of aceclofenac.

Disclosure statement

No potential conflict of interest was reported by the authors.