In situcomposite 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 2 2 4 1 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.

Formulation and optimization of gellan gum-poloxamer based dexamethasone mucoadhesive in situ gel

“…pH is a very important factor for buccal formulations. The normal physiological pH of the buccal mucosa ranges from 5.5-7.5 [17,18]. The pH of all in situ gel formulations containing DEX was observed in the range of 6.72-6.82 (Table 1).…”

“…As anticipated due to its thermoresponsiveness, at 37±0.1ºC all of the preparations showed non-Newtonian pseudoplastic flow, as is expected for Plx above the sol-gel transition temperature. It is precisely the non-Newtonian pseudoplasticity flow that is beneficial in buccal application, as it causes the gel to break down and disperse over the oral mucosa and then after being applied it regains its initial structure [18,[23][24][25]. In addition, at 25±0.1ºC the formulations demonstrated Newtonian flow.…”

“…For drug delivery it is ideal for the in situ gel to be sol state at room temperature, thereby facilitating administration of the drug, and then for the formulation to rapidly form a gel when in the oral cavity. Moreover, these gels should not dissolve, but rather remain in the gel form for a length of time [18].…”

A Comprehensive Review on in Situ Gels

“…An aqueous solution of gellan dropped into the eye undergoes a transition into the gel state due to the temperature and ionic condition (Ca +2 ) in the tear fluid. Drug release from these in situ gels prolonged due to longer pre-corneal contact times of the viscous gels compared with conventional eye drops [90,91].…”

Approaches to the Selection of Excipients for Dental Gel With Cetylpyridinium Chloride

“…В составе гелей стоматологических, цетипиридиния хлорид (0,1%) представлен только в комбинации с лидокаина гидрохлоридом в составе местноанестезирующих средств, назначаемых детям при прорезывании зубов [3,9]. В настоящее время известно большое число исследований, посвященных разработке гелей стоматологических с субстанциями синтетического и природного происхождения, в том числе с антимикробными свойствами [10][11][12][13][14][15][16][17][18][19][20]. Существуют и работы по изучению местных адгезивных ЛФ с цетилпиридиния хлоридом [9,[21][22][23][24][25].…”