Abstract
Objective: The objective of the present investigation was to improve the solubility and dissolution rate of poorly soluble drug meloxicam by its ternary inclusion complexation with natural polymers and beta-cyclodextrin (β-CD) by kneading.
 Methods: Equimolar physical mixture (1:1) was prepared by homogeneously kneading drug and β-CD using a solution of agar and pectin in water to get a paste, then paste was dried overnight to get inclusion complex. Inclusion complex was evaluated for drug content, the yield of the adsorption process, Fourier-transform infrared (FTIR), differential scanning calorimeter (DSC), powder X-ray diffractometry (PXRD), scanning electron microscopy (SEM), dissolution, and stability studies.
 Results: The phase solubility diagrams exhibit AL showing a linear increase of drug solubility and indicating the formation of soluble complexes. The FTIR and DSC show compatibility between meloxicam and β-CD, while slight broadening in the peak with a reduction in intensity and early onset indicates the reduction in drug crystallinity which confirms in PXRD pattern. The SEM of binary, as well as ternary, showed no aggregation, and there was a gap between the particles also indicating good redispersibility. The dissolution rate of the drug from the kneaded ternary complex with pectin was significantly rapid compared with the pure drug. The maximum drug release was observed at 85.21±1.84% at the end of 60 min. The ternary complex was found stable after 3 months stability studies.
 Conclusion: The results indicated that ternary inclusion complexation with natural polymers and β-CD was most useful for enhancement of solubility and dissolution rate of a poorly soluble drug like meloxicam.
Highlights
Cyclodextrin inclusion complexes play an important role in improving the therapeutic efficacy of drugs with poor solubility and/or stability problems
The results indicated that ternary inclusion complexation with natural polymers and β-CD was most useful for enhancement of solubility and dissolution rate of a poorly soluble drug like meloxicam
The stability constant (Ks) computed from the slope and intercept of the phase solubility diagram was found to be 587.24 M−1, 912.23 M−1, and 1021.58 M−1 in case of the binary system, ternary system with agar, and ternary system with pectin indicating an increase in stability constant value of ternary system compared to the binary system
Summary
Cyclodextrin inclusion complexes play an important role in improving the therapeutic efficacy of drugs with poor solubility and/or stability problems. Instead of attempting only binary inclusion complex addition of small amounts of water-soluble polymers to the system, which causes an increase in solubilization efficiency and may result in reducing amounts of CD [10,11]. These results can be attributed to the synergistic effect of polymer and CD solubilization on the formation of drug: CD:water-soluble polymer ternary complexes [12,13]. There are different types of the hydrophilic polymer have been tried including synthetic and semi-synthetic, but there was a rare use of natural polymer for this purpose [22]
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