Development of Oral In Situ Gelling Liquid Formulations of Garcinia Extract for Treating Obesity

Abstract

Novel in situ gelling liquid formulations incorporating garcinia extract were developed to achieve prolonged delivery of hydroxycitric acid (HCA), an active compound displaying anti-obesity function, following oral administration. The optimized formulation was composed of sodium alginate (1.5% w/v), hydroxypropyl methylcellulose (HPMC K100) (0.25% w/v), calcium carbonate (1% w/v) and garcinia extract (2% w/v). The formulation displayed rapid gelation in less than a minute on exposure to 0.1 N hydrochloric acid (pH 1.2) and remained afloat for more than 24 h. The formulations were capable of gradually releasing more than 80% of HCA load over 8 h, depending on the composition. The resulting gels exhibited high values of gel strength by texture analysis, suggesting they would offer resistance to breakdown under the action of stomach content movement. The optimized formulation loaded garcinia extract significantly reduced lipid accumulation in 3T3-L1 adipocyte cells and displayed moderate anti-inflammatory activity by inhibiting the production of nitric oxide (NO) in LPS-stimulated RAW 264.7 macrophage cells. These findings demonstrate that oral in situ gelling liquid formulations based on sodium alginate and HPMC K100 offer much potential for sustained delivery of HCA and other anti-obesity compounds.

Design and development of gastro-retentive gel forming system comprising curcumin loaded Nanostructured lipid carrier for stomach specific delivery

“…The maximum loaded at gel fracture was denoted as gel strength. Each formulation was measured in triplicate and the results were reported [25].…”

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“…Fungfoung et al formulated an oral hydroxycitric acid (HCA) containing in situ gelling liquid, combining sodium alginate as a gelling polymer, with calcium carbonate as a cross-linker, and HPMC K100. The formulation presented a rapid gelation time of less than a minute in a solution containing 0.1 N of HCl, gradually released the API within 8 h, and had a floating time of more than 24 h [ 29 ]. Similarly, Sharma et al created an oral spiramycin-containing in situ gelling formulation with HPMC and sodium alginate.…”

“…Single-unit floating system Layered pellets obtained in a fluidized bed processor Tablets obtained by wet granulation Tablets obtained by direct compression Tablets or capsular devices fabricated by HME/semi-solid extrusion coupled with FDM In situ gelling liquid formulation [23][24][25][26][27][28][29][30] Multiple-unit floating system Granules with APIs obtained by wet granulation Foaming encapsulated particles prepared by ultrasonic batch technology Mini-tablets with encapsulated microparticles, prepared by direct compression [23,[31][32][33][34]…”