Development and evaluation of drug-cyclodextrin-polymer ternary system of Cefuroxime axetil to enhance the solubility and dissolution efficiency

Abstract

Cefuroxime axetil (CA) is BCS class II drug and has 55% absolute oral bioavailability due to poor aqueous solubility hence the present work is an attempt to enhance the solubility and hence dissolution of CA by inclusion complexation with natural Cyclodextrins (CDs). The complexation efficiency of Cyclodextrin is low and hence large amount of CDs are required to solubilize small amount of poorly water-soluble drug. To overcome this limitation the hydrophilic polymers were used to improve the complexation efficiency of cyclodextrin through the formation of ternary complexes. In association with water soluble polymers like Polyvinyl Pyrrolidone (PVP) and Hydroxy Propyl Methyl Cellulose (HPMC) the complexation potential CDs (β-CD and HP-β-CD) was found to be improved which was analyzed by comparative evaluation of binary (drug: cyclodextrin) and ternary system (drug:cyclodextrin:polymer). Binary and ternary complexes were prepared by lyophilization method. On the basis of physicochemical characterization techniques like TLC, FTIR, DSC, and XRPD, the complex formation between CA, CD and water-soluble polymers was confirmed. The dissolution rate studies were also carried out in order to assess the in-vitro performance of complexes. Drug-HP-β-CD-HPMC lyophilized system showed higher solubility and dissolution rate as compared to other systems.

Characterization, Stability, and Antibrowning Effects of Oxyresveratrol Cyclodextrin Complexes Combined Use of Hydroxypropyl Methylcellulose

“…It has been proved that the addition of hydroxypropyl methylcellulose (HPMC) helps to enhance the storage stability [ 30 ] and the activity of some lipophilic molecules, such as resveratrol and piperine [ 31 , 32 ]. There are also some reports that HPMC can be used as a mediator to enhance the complexation efficiency of CD to guest molecules [ 33 , 34 ]. Compared with the binary system, the formed guest-molecule–CD–polymer ternary system may help to achieve better physical and chemical properties of the guest molecule, such as antioxidant and antibacterial activities [ 31 , 32 ].…”

“…In our literature survey, there were also no published reports on the ternary inclusion of Oxy with CD–polymers. Based on the previous reports on the role of HPMC in the ternary system [ 33 , 34 ], it is speculated that the presence of HPMC will further enhance the complexing ability of CD and Oxy, thereby improving the stability of Oxy in solution, and will not adversely affect the antibrowning activity of Oxy. To investigate the effect of HPMC on the Oxy–CD binary system and to evaluate the possible effect of complexation on the stability and antibrowning activity of Oxy, we have therefore interrogated the features of Oxy–CD, Oxy–HPMC, and Oxy–CD–HPMC solutions, and present data which indicate that using HPMC as the third component to improve the stability of the Oxy and β-CD or HP–β-CD inclusion complex (Oxy–β-CD and Oxy–HP–β-CD) in solution without influence its antibrowning activity to fresh-cut apple slices.…”