Inhibition of the pro-inflammatory mediators in rat neutrophils by shanzhiside methyl ester and its acetyl derivative isolated from Barleria prionitis.

ETHNOPHARMACOLOGICAL RELEVANCE: The aerial parts of Barleria prionitis Linn. (BP) (Acanthaceae) plant has long been used to treat inflammatory disorders such as toothache, swellings, arthritis and gout. AIM OF THE STUDY: The purpose of this study was to evaluate the effects of shanzhiside methyl ester (SME), 8-O-acetyl shanzhiside methyl ester (ASME) and iridoid glycosides rich monoterpenoidal fraction (IFBp), isolated from the aerial part of BP, on the pro-inflammatory mediators in stimulated rat neutrophils. MATERIALS AND METHODS: Rat neutrophils were incubated with or without test drugs. The influence of laboratory isolated and identified SME, ASME and IFBp on the production and release of pro-inflammatory mediators i.e. myeloperoxidase (MPO), elastase, matrix metalloproteinase-9 (MMP-9), interleukin 8 (IL-8), tumor necrosis factor alpha (TNF-α) and leukotriene B4 (LTB4) was evaluated in the formyl-met-leu-phenylalanine (f-MLP) and lipopolysaccharide (LPS) stimulated rat neutrophils using enzyme-linked immunosorbent assay (ELISA) methods. IFBp was also standardized with the high performance thin layer chromatography by simultaneous determination of SME and ASME marker compounds. RESULTS: SME, ASME and IFBp displayed concentration-dependent inhibitory effects on the MPO, elastase and MMP-9 enzymes release, and IL-8, TNF-α and LTB4 cytokines production in the f-MLP and LPS stimulated rat neutrophils. The content of SME and ASME was found to be 17.32 ±â€¯1.98 and 11.30 ±â€¯1.06% w/w, respectively, in IFBp by HPTLC method. CONCLUSION: Altogether, the present results suggest that the iridoidal glycosides of BP may be considered as therapeutic strategy against neutrophil-mediated inflammatory diseases. Developed and validated HPTLC method for the standardization of IFBp of BP can be used as a quality control tool for the routine qualitative and quantitative analysis of Barleria species containing SME and/or ASME.

Solid State Characterization of Domperidone: Hydroxypropyl-ß-Cyclodextrin Inclusion Complex.

The purpose of the present study was to prepare inclusion complex of domperidone with hydroxylpropyl-ß-cyclodextrin in order improved the solubility and hence to increase dissolution of domperidone. An effect of concentration of hydroxylpropyl-ß-cyclodextrin on the aqueous solubility of domperidone was determined by phase-solubility method. The aqueous solubility of domperidone increased as a function of hydroxylpropyl-ß-cyclodextrin concentration, showing AL type diagram. Solid domperidone/hydroxylpropyl-ß-cyclodextrin complex was prepared in ratio 1:1 by ultrasonication and kneading method. Solid state inclusion complex was characterized by FTIR, powder X-ray diffraction and differential-scanning calorimetry techniques. FTIR studies showed intactness of drug in complex whereas powder diffraction studies showed that hydroxylpropyl-ß-cyclodextrin complex was amorphous. Solubility studies showed that complexation increased domperidone solubility as compared to pure drug in 0.1M hydrochloric acid and distilled water. Drug content confirms that ultrasonication is one of the efficient methods to prepare inclusion complex. Dissolution data of inclusion complexes also indicated that there is 1.4 folds increase in dissolution as compared to pure drug and was observed in case of inclusion complexes prepared by ultrasonication.

Intranasal mucoadhesive buspirone formulation: in vitro characterization and nasal clearance studies.

Oral administration is unsuitable for drugs prone to extensive first-pass metabolism, like buspirone. Thus, in the present study an attempt has been made to develop a mucoadhesive intranasal formulation improving permeation characteristics of buspirone HCl. Nasal formulations containing different concentrations of chitosan HCl and hydroxypropyl-beta-cyclodextrins (HP-beta-CD) were prepared and compared with control buspirone HCl solution regarding permeability, in vitro duration of mucoadhesion, in vivo nasal clearance in rats and in vitro cytotoxicity on cell culture. Nearly two fold increase in buspirone permeation was observed with 1% chitosan HCl and a 3.5 fold increase with 1% chitosan HCI and 5% HP-beta-CD. Nasal clearance studies showed retention of 50% radioactivity up to about 3.5 h for formulation F7 containing 1% chitosan HCI compared to 1.5 h for control buspirone solution (F1). Results conclusively demonstrated enhancement in permeation with no cytotoxicity. Thus formulations can be used to improve bioavailability of buspirone HCl.

Absence of wild poliovirus circulation among healthy children in a rural area with high oral poliovirus vaccination coverage.

Poliovirus circulation in a rural community was studied by a stool sample survey. No acute paralytic poliomyelitis case had been reported from the study area during the previous 5 months. Immunization coverage in age groups 7 to 12 months and 12 to 60 months was 95.8 and 94 per cent, respectively. Of the 257 children from whom stool samples were collected (about 6% of the child population), 161 (62.6%) were positive for virus isolation. Poliovirus was isolated from 60 (23.3%) children. All three poliovirus types were detected (41 type 1, 16 type 2 and 3 type 3). Intratypic differentiation tests classified these isolates as vaccine-like. Among the children excreting poliovirus, the proportion of those who did not receive polio vaccine within 30 days prior to the sample collection was 46.3, and 68.7 per cent for poliovirus type 1 and 2, respectively. It was concluded that these poliovirus excreting children were infected by the vaccine strains circulating in the environment. The survey showed that wild poliovirus was not detectable within five months after the last case of acute poliomyelitis. Displacement of the wild virus from the environment and circulation of vaccine virus was achieved by high vaccination coverage in this area.