Antiobese effects of capsaicin-chitosan microsphere (CCMS) in obese rats induced by high fat diet.

Chitosan (CTS) and capsaicin (CAP) are two kinds of effective ingredients for antiobesity, which are extracted from crab shells and Capsicum annuum. However, the strong taste of CAP makes it difficult to consume, and the antiobesity ability of CTS is limited. In this study, we prepared capsaicin-chitosan microspheres (CCMSs) by ion-cross-linking and spray drying and examined the antiobesity ability of CCMSs in obese rats. The effects of CCMSs on body weight, Lee's index, body fat, and serum lipids were investigated. The mRNA expression of PPARα, PPARγ, leptin, UCP2, GPR120, FTO, and adiponectin in the liver was determined by quantitative real-time PCR, and the protein expression of adiponectin, leptin, PPARα, UCP2, and hepatic lipase in serum was evaluated by enzyme-linked immunosorbent assay. CCMSs were prepared with 85.17% entrapment efficiency and 8.87% mean drug loading. Compared with chitosan microspheres, CAP, and Orlistat, the CCMSs showed better ability to control body weight, body mass index, organ index, body fat, proportion of fat to body weight, and serum lipids. The CCMSs upregulated the expressions of PPARα, PPARγ, UCP2, and adiponectin and downregulated the expression of leptin. CCMSs may thus be considered novel, safe, effective, and natural weight loss substances, and there is an additive effect between CTMS and capsaicin.

The preparation of capsaicin-chitosan microspheres (CCMS) enteric coated tablets.

This study aimed to research the preparation and content determination of capsaicin-chitosan microspheres (CCMS) enteric coated tablets. The core tablets were prepared with the method of wet granulation. Nine formulae were designed to determine the optimal formula of the core tablet. Eudragit L100 was used to prepare the CCMS enteric-coated tablets. The effect of enteric coated formulation variables such as content of talc (10%, 25% and 40%), plasticisers (TEC and DBS), dosage of plasticiser (10%, 20% and 30%) and coating weight (2%, 3% and 5%) were evaluated for drug release characteristics. The in vitro release was studied using 0.1 N HCl and pH 6.8 phosphate buffer. Enteric coated tablets without ruptures or swelling behaviour over 2 h in 0.1 N HCl indicated that these tablets showed acid resistance. The accumulated release rate in phosphate buffer (pH 6.8) revealed that the prepared tablets were able to sustain drug release into the intestine and a first-order release was obtained for capsaicin. This research is the first report of the preparation and content determination of CCMS enteric coated tablets. The sustained release behavior of enteric coated formulations in pH 6.8 phosphate buffer demonstrated that it would be a potential drug delivery platform for sustained delivery of gastric irritant drugs.

Preparation of Chitosan and Water-Soluble Chitosan Microspheres via Spray-Drying Method to Lower Blood Lipids in Rats Fed with High-Fat Diets.

This experiment aimed to investigate the effects of the chitosan (CTS) and water-soluble chitosan (WSC) microspheres on plasma lipids in male Sprague-Dawley rats fed with high-fat diets. CTS microspheres and WSC microspheres were prepared by the spray-drying technique. Scanning electron microscopy (SEM) micrographs showed that the microspheres were nearly spherical in shape. The mean size of CTS microspheres was 4.07 µm (varying from 1.50 to 7.21 µm) and of WSC microspheres was 2.00 µm (varying from 0.85 to 3.58 µm). The rats were classified into eight groups (n = 8) and were fed with high-fat diets for two weeks to establish the hyperlipidemic condition and were then treated with CTS microspheres and WSC microspheres, CTS and WSC for four weeks. The results showed that CTS and WSC microspheres reduced blood lipids and plasma viscosity and increased the serum superoxide dismutase (SOD) levels significantly. This study is the first report of the lipid-lowering effects of CTS and WSC microspheres. CTS and WSC microspheres were found to be more effective in improving hyperlipidemia in rats than common CTS and WSC.

Effects of chitosan and water-soluble chitosan micro- and nanoparticles in obese rats fed a high-fat diet.

PURPOSE: This study determined the effects of chitosan (CTS) and water-soluble chitosan (WSC) microparticles (MPs) and nanoparticles (NPs) in rats with high-fat diet-induced obesity. METHODS: THE RATS WERE RANDOMLY SEPARATED INTO EIGHT GROUPS: a normal diet group (the blank control), a high-fat emulsion group (the negative control), CTS and WSC control groups, CTS-MP and WSC-MP groups, and CTS-NP and WSC-NP groups. All groups (except the blank control group) were fed the high-fat diet for 4 weeks to establish the obesity model. Different samples were administered orally once daily to the treatment groups for 4 weeks. RESULTS: A significantly lower weight gain was observed in the WSC-MP and WSC-NP groups, as well as in the CTS-MP and CTS-NP groups, compared with rats given a normal diet and a high-fat diet (P < 0.05). The WSC-MP rats had the least weight gain among all the groups. The food intake in the eight groups had the same trend as weight gain. CTS and WSC MPs and NPs significantly reduced the final amounts of epididymal and perirenal white adipose tissue. Liver weight was reduced in the CTS-MP group compared to rats fed a high-fat diet. Serum total cholesterol and low-density lipoprotein cholesterol were significantly reduced in all treatment groups, with the WSC-MP and CTS-MP groups showing a more significant reduction than the other groups. Triacylglycerol levels were significantly reduced in the WSC-NP group compared to the high-fat group. The mortality rates of CTS-MP, CTS-NP, WSC-MP, and WSC-NP groups were 30%, 30%, 55%, and 65%, respectively. The median lethal dose for the WSC-MP and WSC-NP groups were 4080 mg/kg and 2370 mg/kg, respectively. CONCLUSION: These results indicate that CTS and WSC MPs and NPs have greater effects than commercially available CTS and WSC, and can be used as potential antiobesity agents.

Hypolipidemic effects of chitosan nanoparticles in hyperlipidemia rats induced by high fat diet.

The aim of this study was to investigate the hypolipidemic effects of chitosan nanoparticles(CTS-NP) preparations with ionotropic gelation, rotary evaporation, and spray-drying technique. Male SD (Sprague-Dawley) rats were separated into five groups, a normal diet group, a high fat emulsions group, a CTS control group and CTS-NP groups treated with two different doses of CTS-NP. The nanoparticles were spherical in shape and had a smooth surface. The size range of the nanoparticles was between 500 and 1000 nm. The apparent serum lipid and plasma viscosity in CTS-NP group was significantly lower than that in the CTS group, as well as the serum superoxide dismutate (SOD) levels was increased. Although no significant difference in adipose tissue was found among the groups, the rats fed on CTS-NP had lower relative liver weight and body weight when compared with those fed on normal diet. This study was the first report of the effects of CTS-NP in the hyperlipidemia rats, and suggests that the CTS-NP could be used for the treatment of hyperlipidemia.