The purpose of the study was to prepare and evaluate the anti-inflammatory activity of cyclodextrin (CD) complex of curcumin for the treatment of inflammatory bowel disease (IBD) in colitis-induced rat model. Inclusion complexes of curcumin were prepared by common solvent and kneading methods. These complexes were further evaluated for increase in solubility of poorly soluble curcumin. The inclusion complexes were characterized for enhancement in solubility, in vitro dissolution, surface morphology, infrared, differential scanning calorimetry, and X-ray studies. Solubility, phase solubility, and in vitro dissolution studies showed that curcumin has higher affinity for hydroxypropyl-β-CD (HPβCD) than other CDs. HPβCD complex of curcumin was further investigated for its antiangiogenic and anti-inflammatory activity using chick embryo and rat colitis model. HPβCD complex of curcumin proved to be a potent angioinhibitory compound, as demonstrated by inhibition of angiogenesis in chorioallantoic membrane assay. Curcumin- and HPβCD-treated rats showed a faster weight gain compared to dextran sulfate solution (DSS) controls. Whole colon length appeared to be significantly longer in HPβCD-treated rats than pure curcumin and DSS controls. An additional finding in the DSS-treated rats was the predominance of eosinophils in the chronic cell infiltrate. Decreased mast cell numbers in the mucosa of the colon of CD of curcumin- and pure-curcumin-treated rats was observed. This study concluded that the degree of colitis caused by administration of DSS was significantly attenuated by CD of curcumin. Being a nontoxic natural dietary product, curcumin could be useful in the therapeutic strategy for IBD patients.

/pdf/effect-of-cyclodextrin-complexation-of-curcumin-on-its-2utqeyoj35.pdf

Effect of Cyclodextrin Complexation of Curcumin on its Solubility and Antiangiogenic and Anti-inflammatory Activity in Rat Colitis Model

The use of cytotoxic chemotherapic agents is the most common method for the treatment of metastatic cancers. Poor water solubility and low efficiency of chemotherapic agents are among the major hurdles of effective chemotherapy treatments. Curcumin and paclitaxel are well-known chemotherapic agents with poor water solubility and undesired side effects. In this study, a novel drug nanocarrier system was formulated by encapsulating curcumin and paclitaxel in poly(β-cyclodextrin triazine) (PCDT) for the therapy of four cancer models; ovarian, lung, prostate, and breast cancer. Cell viability and colony formation assays revealed enhanced curcumin cytotoxicity upon complexation. Annexin V apoptotic studies showed that the PCDT complexation improved curcumin induced apoptosis in human ovarian cancer cell lines A2780 and SKOV-3, human nonsmall cell lung carcinoma cell line H1299, and human prostate cancer line DU-145, while no significant effect was observed with paclitaxel/PCDT complexation. The bioactivity of combining curcumin and paclitaxel was also investigated. A synergism was found between curcumin and paclitaxel, particularly when complexed with PCDT on A2780, SKOV-3, and H1299 cancer cell lines.

Synergistic interaction of paclitaxel and curcumin with cyclodextrin polymer complexation in human cancer cells.

Enhancement of norfloxacin solubility via inclusion complexation with β-cyclodextrin and its derivative hydroxypropyl-β-cyclodextrin

Lovastatin-producing endophytic fungus isolated from a medicinal plant Solanum xanthocarpum.

Aspergillus sp. is known to produce cholesterol reducing drug lovastatin. Limited investigations have been made on screening of high yielding strains from hitherto under-utilized natural sources. With this objective, in the present study, various fungal cultures (130 in number) were isolated from natural sources such as (soil from paddy fields, oyster mushroom beds from the fields and compost) from different regions of interiors of Karnataka and Tamil Nadu of India. All the isolates were identified through standard microbiological methods such as morphological, microscopic methods. These isolates were further cultured for the production of lovastatin through submerged fermentation process (SmF). The extract from each of the isolate was subjected to three replicates of UV spectrophotometry quantification (200-350 nm). Confirmation of the metabolite production was achieved through HPLC and Attenuated total reflectance (ATR-FTIR) chromatography using the drug lovastatin (Biocon Laboratories) as standard. Out of all, nine high lovastatin yielding fungal strains were selected by applying selection pressures. Submerged state fermentation (SmF) extract (lovastatin) of these strains also exhibited the maximum zone of inhibition (≥ 10 mm) against Neurospora crassa (MTCC-790) in bioassay. Fungal strains giving maximum yield of lovastatin were found to be Aspergillus terreus (SSM4) from oyster mushroom bed source that produced a maximum yield of lovastatin (996.6 mg/l) followed by Aspergillus terreus (SSM3) from compost source (900 mg/l), Aspergillus flavus (SSM8) from compost source (643 mg/l). High yielding Aspergillus terreus (SSM4) isolate was characterized by β2 tubulin gene sequencing, confirmed through phylogenetic and molecular evolutionary analyses using MEGA version 5 software. The present study isolated three high lovastatin yielding fungal isolates from natural samples and one of the highest yielding isolate was sequenced and deposited in the MTCC (IMTECH) Chandigarh with issued accession number Aspergillus terreus nhceup 11045.

/pdf/screening-and-molecular-characterization-of-natural-fungal-4xdh1je6pj.pdf

Screening and Molecular Characterization of Natural Fungal Isolates Producing Lovastatin

Several attempts have been made to improve the solubility of water insoluble drugs. Over the years, inclusion complexation of drugs with ?-cyclodextrin has emerged as a viable attempt to improve the dissolution of water insoluble drugs. The aim of the present work was to improve the dissolution rate of lovastatin, a water insoluble drug, by inclusion complexation with ?-cyclodextrin. The stoichiometric ratio determined by phase solubility analysis for inclusion complexation of lovastatin with ?-cyclodextrin was 1:1. The solubility of lovastatin increased with increasing amount of ?-cyclodextrin in water. Gibbs free energy (?G tr °) values were all negative, indicating the spontaneous nature of lovastatin solubilization. Complexes of lovastatin were prepared with ?-cyclodextrin by various methods such as kneading, coevaporation and physical mixing. The complexes were characterized by Fourier-transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction (XRD) patterns. These studies indicated the inclusion of lovastatin in the cavity of ?-cyclodextrin. The complexation resulted in a marked improvement in the solubility of lovastatin. The complex prepared by kneading method showed fastest and highest in vitro dissolution rate compared to the tablets of pure of lovastatin. Physical mixture of ?-cyclodextrin/lovastatin also showed significant improvement in the dissolution rate compared to pure lovastatin. Mean dissolution time (MDT) of lovastatin decreased significantly after preparation of complexes and physical mixture of lovastatin with ?-cyclodextrin. Similarity factor ( f 2 ) indicated significant difference between the release profiles of lovastatin from complexes and from pure lovastatin. Key words: Lovastatin, ?-cyclodextrin, inclusion complexation, in vitro dissolution studies. 

Dhaka Univ. J. Pharm. Sci. 6(1): 25-36, 2007 (June)

The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

/pdf/preparation-and-evaluation-of-inclusion-complex-of-the-lipid-el0rl9wy23.pdf

Preparation and Evaluation of Inclusion Complex of the Lipid Lowering Drug Lovastatin with β-Cyclodextrin

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Preparation and Evaluation of Inclusion Complex of the Lipid Lowering Drug Lovastatin with β-Cyclodextrin