Design and Optimization of Curcumin–HPβCD Bioadhesive Vaginal Tablets by 23 Factorial Design: In Vitro and In Vivo Evaluation

Hani, Umme; Shivakumar, H. G.; Srivastava, Atul; Mahammed, Nawaz; Thirumaleshwar, Shailesh; Varma, Naga Sravan Kumar; Vaghela, Rudra; Shinde, Chetan G.; Gowrav, M P

doi:10.1007/s12247-014-9203-4

Cited by 14 publications

(12 citation statements)

References 23 publications

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“…11 In brief, CTZ (0.3448 g) and HPbCD (1.54 g) in a 1 : 1 molar ratio were ground in a mortar for 1 h with a small quantity of alcohol. 11 In brief, CTZ (0.3448 g) and HPbCD (1.54 g) in a 1 : 1 molar ratio were ground in a mortar for 1 h with a small quantity of alcohol.…”

Section: Preparation Of Ctz-hpbcd Complexmentioning

confidence: 99%

“…A physical mixture of CTZ-HPbCD complexes was prepared using a kneading method based on the previous report by Hani et al with minor modications. 11 In brief, CTZ (0.3448 g) and HPbCD (1.54 g) in a 1 : 1 molar ratio were ground in a mortar for 1 h with a small quantity of alcohol. A thick slurry of the mixture was prepared by intermittently adding distilled water.…”

Section: Preparation Of Ctz-hpbcd Complexmentioning

confidence: 99%

“…CDs are macrocyclic oligosaccharides with six to eight a-D-glucopyranose units linked by (a-1,4) glycosidic bonds, possessing the unique molecular structure of a lipophilic inner and hydrophilic outer surface. 10,11 Recently, Tonglairoum et al 12 reported that a CTZ composite electrospun blend of hydroxypropyl-b-cyclodextrin (HPbCD) with polyvinylpyrrolidone (PVP) exhibited rapid in vitro antifungal activity attributed to enhanced dissolution of clotrimazole. 7 Given the presence of a large number of hydrogen atoms, CDs are widely employed as versatile complexing agents in pharmaceutical formulation design, including their primary use as solubilizers for poorly water-soluble drugs, leading to a corresponding increase in bioavailability with reduced side effects and drug-associated toxicity.…”

Section: Introductionmentioning

confidence: 99%

“…8 In addition, CDs and their derivatives have also been used for the development of assemblies with higher drug loading efficiency, 9 which reduces gastrointestinal irritation and in the development of mucoadhesive tablets. 10,11 Recently, Tonglairoum et al 12 reported that a CTZ composite electrospun blend of hydroxypropyl-b-cyclodextrin (HPbCD) with polyvinylpyrrolidone (PVP) exhibited rapid in vitro antifungal activity attributed to enhanced dissolution of clotrimazole. In addition, the CTZ-PVP/HPbCD complex also reduced the cytotoxicity associated with drug exposure.…”

Section: Introductionmentioning

confidence: 99%

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Design and optimization of clotrimazole–hydroxypropyl-β-cyclodextrin bioadhesive vaginal tablets using Anacardium occidentale gum by 3² factorial design

2015

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Clotrimazole (CTZ), a BCS class II drug, is widely employed in the treatment of vaginal candidiasis. However, due to its poor solubility, repeated administrations are required to maintain a therapeutic concentration. To increase its aqueous solubility, it was complexed with hydroxypropyl-b-cyclodextrin (HPbCD) and formulated as vaginal tablets using natural Anacardium occidentale gum in combination with Carbopol 934P. The formation of a drug-HPbCD complex was confirmed by characterization techniques, viz., scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), 1 H NMR and Fourier transform infrared spectroscopy (FT-IR) studies. Furthermore, 3 2 factorial design was employed to optimize the gum and Carbopol 934P concentrations in the development of CTZ-HPbCD vaginal tablets. In vitro analysis revealed the higher susceptibility of Candida albicans strains and significant mucoadhesion of the tablet formulation. Based on our findings, combined with Anacardium occidentale gum, the CTZ-HPbCD complex could be used for treating fungal infections, and it offers the great advantage of the higher solubility of CTZ with the therapeutic importance of higher bioavailability at the site of action. In addition, the use of natural polymers could also serve to minimize drug toxicity, which would be particularly useful for treating vaginal candidiasis safely in pregnancy.

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Section: Preparation Of Ctz-hpbcd Complexmentioning

confidence: 99%

Section: Preparation Of Ctz-hpbcd Complexmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Design and optimization of clotrimazole–hydroxypropyl-β-cyclodextrin bioadhesive vaginal tablets using Anacardium occidentale gum by 3² factorial design

2015

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“…4A). Hani et al showed a similar melting point for CUR in a complex of CUR and hydroxypropyl-cyclodextrin 40 . In PVP, a peak at ~ 75 ° C was observed which was ascribed to the water loss (Fig.…”

Section: Ftir Analysismentioning

confidence: 89%

Characterization of PVPK90 core shell nanofibers containing curcumin prepared by emulsion electrospinning process

Kamali

Farzadnia

Movaffagh

et al. 2021

Preprint

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The pharmacological effects of curcumin (CUR) as a polyphenolic ingredient of turmeric affected by its water insolubility, poor bioavailability, and instability. The electrospun nanofibers of hydrophilic biodegradable polymer can be addressed this issue. The current study aimed to investigate the CUR-loaded core-shell PVPK90 nanofibers generated from O/W nanoemulsions. CUR-loaded PVPK90 fibers were prepared based on the central composite design and different levels of drug concentration, flow rate, amount of acetone, and organic phase percentage by electrospinning technique and their diameter and uniformity, tensile strength, wetting and disintegration time were evaluated. Then, DSC, FTIR, XRD, TEM, fluorescence microscopy, and drug release test were carried out on the optimized nanofibers. The formulation containing 6 mg/mL CUR, 30% organic phase, 0.4 mL acetone, and flow rate of 1 mL/h was selected as optimum formulation. The results were confirmed the core-shell bead-free uniform fibers at the nanometer scale. The optimum nanofiber showed a good flexibility, short wetting and disintegrating times as well as the amorphous structure. The drug release pattern indicated the rapid release of the drug within 30 min. Our findings confirm that the O/W emulsion electrospinning-based PVPK90 core-shell nanofiber would be beneficial as a novel delivery system for water insoluble drug.

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23 Full Factorial Design for Formulation and Evaluation of Floating Oral In Situ Gelling System of Piroxicam

et al. 2020

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Design and Optimization of Curcumin–HPβCD Bioadhesive Vaginal Tablets by 23 Factorial Design: In Vitro and In Vivo Evaluation

Cited by 14 publications

References 23 publications

Design and optimization of clotrimazole–hydroxypropyl-β-cyclodextrin bioadhesive vaginal tablets using Anacardium occidentale gum by 3² factorial design

Design and optimization of clotrimazole–hydroxypropyl-β-cyclodextrin bioadhesive vaginal tablets using Anacardium occidentale gum by 3² factorial design

Characterization of PVPK90 core shell nanofibers containing curcumin prepared by emulsion electrospinning process

23 Full Factorial Design for Formulation and Evaluation of Floating Oral In Situ Gelling System of Piroxicam

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Design and Optimization of Curcumin–HPβCD Bioadhesive Vaginal Tablets by 23 Factorial Design: In Vitro and In Vivo Evaluation

Cited by 14 publications

References 23 publications

Design and optimization of clotrimazole–hydroxypropyl-β-cyclodextrin bioadhesive vaginal tablets using Anacardium occidentale gum by 32 factorial design

Design and optimization of clotrimazole–hydroxypropyl-β-cyclodextrin bioadhesive vaginal tablets using Anacardium occidentale gum by 32 factorial design

Characterization of PVPK90 core shell nanofibers containing curcumin prepared by emulsion electrospinning process

23 Full Factorial Design for Formulation and Evaluation of Floating Oral In Situ Gelling System of Piroxicam

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Design and optimization of clotrimazole–hydroxypropyl-β-cyclodextrin bioadhesive vaginal tablets using Anacardium occidentale gum by 3² factorial design

Design and optimization of clotrimazole–hydroxypropyl-β-cyclodextrin bioadhesive vaginal tablets using Anacardium occidentale gum by 3² factorial design