Design, Development and Characterzation of Applied Crystal Enginerring on Budesonide Co-Crystal Loaded in Topical Gel.

Abstract

Introduction: The present research work was conducted on poorly aqueous  soluble drug Budesonide with 4-Hydroxybenzoic acid co-crystal. Co-crystallization is  a viable strategy to improving the solubility of weakly water-soluble medicines. Budesonide (BUD) is a crystalline corticosteroid essential in the management of inflammatory dermatitis, including psoriasis, Budesonide (BUD) cocrystal is a novel formulation that exhibit  improved aqueous solubility, the co-former selection is important step in co-crysatallisation it can be selected by different method hydrogen bond theories, pKa-based models, using the solvent evaporation method to produce co-crystals . The combining of Budesonide with a 4 hydroxy benzoic acid to form a new crystalline solid with improved physicochemical properties, including durability, dispersible, absorption and efficacy, while sustaining the therapeutic effect of the Budesonide characterisation peak is determined by Fourier transformed infrared spectroscopy, melting point is determined by Scanning electron microscopy (SEM),Differential scanning calorimetry (DSC) and X- ray diffraction (XRD)obtained particle size of co-crystal. Formulated  co-crystal loaded in Topical gel. The formulated Batch of F6 show better permeability , viscosity and PH and Drug release.

Objectives: The Goal of these study is enhance the ability to dissolve substance BCS II along with class IV,  of medicament eveloping new drugs, poor water solubility and low oral bioavailability pose significant challenges

Methods: BUD co-crystal established Using the solvent evaporation method. The synthesis of co-crystal different six co-former selected according to GRASS system  such as Saccharin, succinic acid, Urea, Para-Amino-benzoic acid (PABA) ,Para- Hydroxy benzoic acid (PHBA), Cinnamic acid  etc. Accurately weighed Equimolar weight of Budesonide and 4-Hydroxy benzoic acid 1:1 ratio was soluble in cosolvent of Ethyl alcohol+ Ethyl acetate .(15)The prepared mixture sonicates till 30 min and transferred into petri plate .keep the prepared solution for 24 hr .dry the product collect the crystalline budesonide i.e. co-crystal of budesonide and stored in airtight tight container .

Results: The Formulated Budesonide co-crystal loaded gel were characterised by Spredability, viscosity ,Exturdability ,Ph , In vitro drug release are determined on the basis of it the optomized batch is selected and futher characterisation of co-crystal is determined by XRD,DSC, SEM and FT-IR .

Conclusions: In the present work, cocrystals of BUD and 4 Hydroxy benzoic acid were prepared using the solvent evaporation technique. The Solid  state characterization of drug and cocrystals was carried out using DSC, XRD,SEM, and FTIR studies BUD cocrystal formation was confirmed. gel using three-level factorial design.. F5 formulation was found to be optimized batch. From the overall conducted study, we can conclude that the newly developed crystalline form of BUD with 4 Hydroxy benzoic acid  showed increased solubility and dissolution rate.