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Cyclodextrin complexes of reduced bromonoscapine in guar gum microspheres enhance colonic drug delivery.

ABSTRACT: Here, we report improved solubility and enhanced colonic delivery of reduced bromonoscapine (Red-Br-Nos), a cyclic ether brominated analogue of noscapine, upon encapsulation of its cyclodextrin (CD) complexes in bioresponsive guar gum microspheres (GGM). Phase-solubility analysis suggested that Red-Br-Nos complexed with β-CD and methyl-β-CD in a 1:1 stoichiometry, with a stability constant (Kc) of 2.29 × 10(3) M(-1) and 4.27 × 10(3) M(-1). Fourier transforms infrared spectroscopy indicated entrance of an O-CH₂ or OCH₃-C₆H₄-OCH₃ moiety of Red-Br-Nos in the β-CD or methyl-β-CD cavity. Furthermore, the cage complex of Red-Br-Nos with β-CD and methyl-β-CD was validated by several spectral techniques. Rotating frame Overhauser enhancement spectroscopy revealed that the Ha proton of the OCH₃-C₆H₄-OCH₃ moiety was closer to the H₅ proton of β-CD and the H₃ proton of the methyl-β-CD cavity. The solubility of Red-Br-Nos in phosphate buffer saline (PBS, pH ∼ 7.4) was improved by ∼10.7-fold and ∼21.2-fold when mixed with β-CD and methyl-β-CD, respectively. This increase in solubility led to a favorable decline in the IC₅₀ by ∼2-fold and ∼3-fold for Red-Br-Nos-β-CD-GGM and Red-Br-Nos-methyl-β-CD-GGM formulations respectively, compared to free Red-Br-Nos-β-CD and Red-Br-Nos-methyl-β-CD in human colon HT-29 cells. GGM-bearing drug complex formulations were found to be highly cytotoxic to the HT-29 cell line and further effective with simultaneous continuous release of Red-Br-Nos from microspheres. This is the first study to showing the preparation of drug-complex loaded GGMS for colon delivery of Red-Br-Nos that warrants preclinical assessment for the effective management of colon cancer.

SUBMITTER: Madan J

PROVIDER: S-EPMC4255741 | biostudies-literature | 2014 Dec

REPOSITORIES: biostudies-literature

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Cyclodextrin complexes of reduced bromonoscapine in guar gum microspheres enhance colonic drug delivery.

Madan Jitender J Gundala Sushma R SR Baruah Bharat B Nagaraju Mulpuri M Yates Clayton C Turner Timothy T Rangari Vijay V Hamelberg Donald D Reid Michelle D MD Aneja Ritu R

Molecular pharmaceutics 20141118 12

Here, we report improved solubility and enhanced colonic delivery of reduced bromonoscapine (Red-Br-Nos), a cyclic ether brominated analogue of noscapine, upon encapsulation of its cyclodextrin (CD) complexes in bioresponsive guar gum microspheres (GGM). Phase-solubility analysis suggested that Red-Br-Nos complexed with β-CD and methyl-β-CD in a 1:1 stoichiometry, with a stability constant (Kc) of 2.29 × 10(3) M(-1) and 4.27 × 10(3) M(-1). Fourier transforms infrared spectroscopy indicated entra ...[more]

PMID: 25350222

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Project description:Mineral precipitation via microbial activity is a well-known process with applications in various fields. This relevance of microbially induced calcite precipitation (MICP) has pushed researchers to explore various naturally occurring MICP capable bacterial strains. The present study was performed to explore the efficiency of microbially induced calcite precipitation (MICP) via locally isolated bacterial strains and role of guar gum, which is a naturally occurring polymer, on the MICP process. The strains were isolated from local soil and screened for urease activity Further, the urease positive strain was subjected to urea and calcium chloride based medium to investigate the efficacy of isolated strain for microbial induced precipitation. Among screened isolates, the soil bacterium that showed urease positive behaviour and precipitated calcium carbonate was subjected to 16S rRNA gene sequencing. This strain was identified as Bacillus velezensis. Guar gum-a natural polymer, was used as a sole carbon source to enhance the MICP process. It was observed that the isolated strain was able to breakdown the guar gum into simple sugars resulting in two-fold increase in calcium carbonate precipitate. Major bio-chemical activities of isolated strain pertaining to MICP such as ammonium ion concentration, pH profiling, and total reducing sugar with time were explored under four different concentrations of guar gum (0.25%, 0.5%, 0.75% and 1% w/v). Maximum ammonium ion concentration (17.5 ?g/ml) and increased pH was observed with 1% guar gum supplementation, which confirms augmented MICP activity of the bacterial strain. Microstructural analysis of microbial precipitation was performed using scanning electron microscopy (SEM) and X-ray diffraction (XRD) techniques, which confirmed the presence of calcium carbonate in different phases. Further, XRD and SEM based studies corroborated that guar gum supplemented media showed significant increase in stable calcite phase as compared to media without guar gum supplementation. Significant diverse group of nitrogenous compounds were observed in guar gum supplemented medium when subjected to Gas Chromatography-Mass spectrometry (GC-MS) profiling.

Dataset Information

Cyclodextrin complexes of reduced bromonoscapine in guar gum microspheres enhance colonic drug delivery.

Publications

Cyclodextrin complexes of reduced bromonoscapine in guar gum microspheres enhance colonic drug delivery.

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