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The objective of the present study was to evaluate the antiobesity potential of various plant (leaves or seed) extracts through a modified in vitro lipase inhibitory activity assay. Dimethyl sulphoxide (DMSO, negative control or solvent) extracts as cold infusion of leaves and seeds of some plants were studied for lipase inhibitory potential using porcine pancreatic lipase enzyme, p-nitro phenyl acetate and orlistat (as positive control or standard inhibitor). Among the leaves, the Urtica dioica showed the best pancreatic lipase inhibition activity (52.0 %). On the other hand, among the seeds, Trachyspermum ammi showed the highest per cent lipase inhibition (91.68 %). Among six leaves' and seven seeds' extract, it was evident that the seeds showed better pancreatic lipase inhibition activity over the leaves in the study. The lipase inhibition was found to be in the range of 34.43 to 91.68 % for the plants in study. DMSO extract of the plants under the study showed significant pancreatic lipase inhibitory activity indicating strong antiobesity activity. Therefore, the plants can be further investigated for the identification and isolation of chief bioactive constituents for developing the lead molecules for obesity treatment. [ABSTRACT FROM AUTHOR]

Cyclodextrins are water-soluble oligosaccharides formed by the action of cyclodextrin glucosyl transferase enzyme (CGTase) on the medium containing starch. Cyclodextrins are proven to be a cost-effective breakthrough in the pharmaceutical industry by formulating them with polymers and drugs to improve the safety, bioavailability, and solubility of APIs. This review describes the current status and advancement of cyclodextrin research in drug delivery. The use of cyclodextrins to improve the solubility and dissolution properties of poor water-soluble products has been reviewed exhaustively with a specific focus on their physicochemical property, practical methods, toxicity, the drug-cyclodextrin compatibility and its applications. [ABSTRACT FROM AUTHOR]

Herbal drug naringenin is well known for its anti-cancer, anti-oxidant, anti-inflammatory activities, as carbohydrate metabolism promoter, immunity system modulator, BCRP/ABCG2 inhibitor, hormone substitute and hormone antagonist since decades. However, use of naringenin as pharmaceutical aid is hindered due to its low aqueous solubility. In the present study, β-cyclodextrin and hydroxy propyl -β- cyclodextrin based biocompatible nanoforms were developed by the exploitation of self-assembly properties of cyclodextrins in aqueous media using sodium dodecyl sulphate and Pluronic F108 as co-surfactants. Prepared formulations were evaluated for various parameters such as particle size, zeta potential, polydispersity index, percent encapsulation efficiency, drug solubility and in vitro permeation studies. Particles present in all the formulations were not greater than the 161.2 nm with surface charge up to -24.8 mV and highest polydispersity index of 0.739. Aqueous solubility of drugs in prepared formulations was increased by 4 fold. Drug permeability was increased twice of free drug naringenin. It was concluded that the cyclodextrin based biocompatible nanosystems can be developed in the improvement of aqueous solubility and hence the bioavailability of herbal drugs. [ABSTRACT FROM AUTHOR]

Delivery of poorly soluble drugs results in poor absorption and low bioavailability to the systemic circulation. Chrysophanol (1,8-dihydroxy 3-methyl anthraquinone) a plant derived herbal drug is well known for its strong anti-inflammatory, anti-mutagenic, and anti-carcinogenic activities but poor aqueous solubility (hence the lower dissolution rate), is a major barrier in its intestinal absorption. To improve the bioavailability and prolong its duration in the body system, its phospholipid complex was prepared and evaluated for various physicochemical parameters like encapsulation efficiency, scanning electron microscopy, differential scanning calorimetry (DSC), X-ray powder diffractometry (X-RPD), IR spectroscopy, aqueous/ n-octanol solubility, and dissolution study. The phospholipid complex of chrysophanol was found, fluffy and porous with rough surface morphology. FTIR, DSC, and X-RPD data confirmed the complex formation. The 89.1 % of chrysophanol was encapsulated in the phospholipid complex. The aqueous solubility of chrysophanol was improved from 0.60 to 30.09 μg ml in the prepared complex. The improved dissolution was shown by the complex (which showed continuous release up to 83.67 % of chrysophanol) at the end of 12 h, in comparison to free drug (which showed a total of only 45.12 % drug release at the end of 12 h of dissolution study). [ABSTRACT FROM AUTHOR]

Developing the drugs as amphiphilic lipid complexes is a potential approach for improving therapeutic efficacy of the drugs by increasing solubility, reducing drug crystallinity, modifying dissolution behavior (sustained or controlled release), and improving bioavailability. Emodin (1,3,8-trihydroxy-6-methylanthraquinone), an anthranoid derivative, shows several biological effects like antimicrobial, antidiuretic, anti-cancerous, and potent antioxidant but due to poor solubility, the dissolution restrains its valuable importance. To overcome this limitation, the emodin-phospholipid complex was developed and investigated by thermal analysis (differential scanning calorimetry), crystallographic (X-ray diffractography), surface morphology (scanning electron microscopy), spectroscopic methods (FT-IR, H-NMR), solubility, and the dissolution (in vitro drug release) study. The phospholipid complex of emodin was found, fluffy and porous with rough surface morphology in the SEM. FT-IR, H-NMR, DSC, and X-RPD data confirmed the formation of the complex. The water and n-octanol solubility of emodin was improved from 2.25 to 9.97 and 53.45 to 77.62 μg/ml, respectively, in the prepared complex. The improved dissolution was shown by the phospholipid complex. Based on the results of the study, it can be concluded that the phospholipid complex may be considered as promising drug delivery system for improving the overall absorption and bioavailability of the emodin molecule. [ABSTRACT FROM AUTHOR]

Hair has psychological and sociological importance throughout the ages in framing the personality and general appearance of an individual. Significant progress is being made on discovering an effective and safe drug for hair growth. Angiogenesis, androgen antagonism, vasodilation, potassium channel opening and 5-alpha reductase inhibition are the major non-surgical therapeutic strategies of hair growth promotion. In spite of a flood of drugs claiming to be useful as hair growth promoters, more rational strategies, which can target the problem areas or stages of the hair growth cycle effectively, are still awaited. This article highlights the developments in hair rejuvenation strategies and reviews the potential of herbal drugs as safer and effective alternatives. [ABSTRACT FROM AUTHOR]

The poor and/or erratic oral bioavailability of polyphenolics can be improved using the PHYTOSOME® 1 [1] PHYTOSOME® is a registered trademark of Indena S.p.A. Milan, Italy. delivery system, a strategy that enhances the rate and the extent of solubilization into aqueous intestinal fluids and the capacity to cross biomembranes. Phospholipids show affinity for polyphenolics, and form supramolecular adducts having a definite stoichiometry. This article reviews the preparation and characterization of PHYTOSOME® complexes and their activity in various medicinal (cardiovascular, anti-inflammatory, hepatoprotective, anticancer) and cosmetic (skin aging) realms of application. [Copyright &y& Elsevier]

Obesity is a growing global health problem, leading to various chronic diseases. Despite standard treatment options, the prevalence of obesity continues to rise, emphasizing the need for new drugs. in vitro methods of drug discovery research provide a time and cost-saving platform to identify new antiobesity drugs. The review covers various aspects of obesity and drug discovery research using in vitro models. Besides discussing causes, diagnosis, prevention, and treatment, the review focuses on the advantages and limitations of in vitro studies and exhaustively covers models based on enzymes and cell lines from different animal species and humans. In contrast to conventional in vivo animal investigations, in vitro preclinical tests using enzyme- and cell line-based assays provide several advantages in development of antiobesity drugs. These methods are quick, affordable, and provide high-throughput screening. They can also yield insightful information about drug-target interactions, modes of action, and toxicity profiles. By shedding light on the factors that lead to obesity, in vitro tests can also present a chance for personalized therapy. Technology will continue to evolve, leading to the creation of more precise and trustworthy in vitro assays, which will become more and more crucial in the search for novel antiobesity medications., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)