ABSTRACT
The study was designed to generate an ophthalmic thermosensitive in situ gel with improved mechanical and mucoadhesive properties that may prolong the retention time to enhance the bioavalability of pearl hydrolyzate. The gene was comprised of poloxamer 407, poloxamer188 and Carbopol 934, which were optimized by central composite design and response surface methodology. The rheological properties, transcorneal permeability, retention time and in vitro release behaviors of the optimal gel formulation were investigated. The gel was Newtonian liquid at 25℃ and performed as a semisolid gel with non-Newtonian liquid property with a gelation time of 13 s at 35℃. Compared with a conventional eye drops, the ophthalmic in situ gel exhibited a sevenfold increase in retention with a sustained release behavior, which was observed with suitable permeability coefficient at 5.58 cm·s-1. In conclusion, the new gel of pearl hydrolyzate prolonged the release duration of drug, which may decrease the frequency of administration of pearl hydrolyzate. kilometers with ecological similarity between 20% and 40%, mainly in Yunnan, Guangxi, Guangdong, Guizhou, Hainan, Sichuan, Fujian and Chongqing. The climate factors mainly affecting the distribution of Panax notoginseng (Burk.) F. H. Chen were precipitation of warmest quarter, SD of temperature seasonality, altitude, isothermality, coefficient of variation of precipitation seasonality, mean temperature of monthly, precipitation of driest month, reference bulk density of soil and soil texture.
ABSTRACT
<p><b>OBJECTIVE</b>To investigate the effect of total alkaloids of Sophora alopecuroides (TASA) on dextran sulfate sodium (DSS)-induced colitis in mice.</p><p><b>METHODS</b>Chronic experimental colitis was induced by administration of 4 cycles of 4% DSS. Fifty mice were randomly distributed into 4 groups (normal, DSS, DSS/high-dose TASA, and DSS/low-dose TASA groups) by a random number table with body weight stratification. Mice in the normal group (n=11) and DSS-induced colitis control group (n=15) received control treatment of 20 mL/kg distilled water; DSS plus TASA high- and low-dose groups (n=12 each) were treated with TASA solution (20 mL/kg) at the doses of 60 mg/kg and 30 mg/kg, respectively. The severity of colitis was assessed on the basis of clinical signs, colon length, and histology scores. Moreover, secretory immunoglobulin A (sIgA) and haptoglobin (HP) were analyzed by enzyme linked immunosorbent assay; intercellular adhesion molecule 1 (ICAM-1) and macrophage-migration inhibitory factor (MIF) gene expressions were analyzed by quantitative reverse transcriptase realtime polymerase chain reaction (qRT-PCR) using SYBA green I; and nuclear factor κ B (NF-κ B) expression and activation and p65 interaction with the promoter of ICAM-1 gene were assessed by Western blotting and chromatin immunoprecipitation assay.</p><p><b>RESULTS</b>TASA administration significantly attenuated the damage and substantially reduced HP elevation and maintained the level of cecum sIgA. TASA inhibited the ICAM-1 gene expression and had no effect on MIF gene expression. Also, TASA was able to reduce phospho-I κ B α (p-I κ B α) protein expression; however, it had no effect on the activation of I κ B kinase α (IKK α) and inhibitor of NF-κ B α (I κ B α). Moreover, TASA inhibited the p65 recruitment to the ICAM-1 gene promoter.</p><p><b>CONCLUSIONS</b>TASA had a protective effect on DSS-induced colitis. Such effect may be associated with its inhibition of NF-κ B activation and blockade of NF-κ B-regulated transcription activation of proinflammatory mediator gene.</p>
Subject(s)
Animals , Female , Mice , Alkaloids , Pharmacology , Therapeutic Uses , Cecum , Metabolism , Pathology , Colitis , Drug Therapy , Pathology , Colon , Pathology , Dextran Sulfate , Down-Regulation , Haptoglobins , Metabolism , I-kappa B Proteins , Metabolism , Immunoglobulin A, Secretory , Metabolism , Intercellular Adhesion Molecule-1 , Genetics , Metabolism , Intestinal Mucosa , Pathology , Macrophage Migration-Inhibitory Factors , Genetics , Metabolism , Mice, Inbred C57BL , NF-KappaB Inhibitor alpha , Phosphorylation , Phytotherapy , Promoter Regions, Genetic , Genetics , Protective Agents , Pharmacology , Therapeutic Uses , Protein Binding , Signal Transduction , Sophora , Chemistry , Transcription Factor RelA , MetabolismABSTRACT
<p><b>OBJECTIVE</b>To prepare colon-targetting tablets of total alkaloids of Sophora alopecuroides and evaluate the effect of pectins of different degree of esterification (DE) on sophoridine release profiles in-vitro.</p><p><b>METHOD</b>Wet granulation technique was employed to prepare petin-based matrix tablets, then tablets were coated the optimal formulation with Kollicoat MAE 30 DP based on the optimal formulation and analysed their release.</p><p><b>RESULT</b>Coated formulation E could target total alkaloids of S. alopecuroides to colon and various DE of pectin exerted different effects on sophoridine release. The release of low DE pectin-based matrix tablets coating with Kollicoat MAE 30 DP approximatedly fitted zere-order eqution, which was erosion depended.</p><p><b>CONCLUSION</b>Low DE pectin-based matrix tablet coating with Kollicoat MAE 30 DP can deliver sophoridine to colon, hence improve the effectiveness of sophoridine.</p>