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Because it can not only directly reach the lesion site to play a local therapeutic effect, but also avoid the liver first pass effect and play a systemic therapeutic effect, vaginal mucosal administration has attracted more and more attention from domestic and foreign scholars in the treatment of vaginitis, cervicitis and other diseases. This article introduces the physiological characteristics of the vagina and discusses the factors affecting drug absorption. The vaginal mucosal drug-administered preparations, which are contained in the drug database of U.S. Food and Drug Administration(FDA) and China Food and Drug Administration(CFDA), and listed in the 2015 edition of Chinese Pharmacopoeia, are taken as the research objects. And the application of their dosage forms, indications and other aspects were sorted out and analyzed. The related literature on vaginal mucosal drug delivery systems in recent years was reviewed, and the dosages forms and in vitro and in vivo evaluation were summarized. Some problems in the study of vaginal mucosal drug preparations have been pointed out:①the western medicine preparations are widely used, and the related Chinese medicine preparations have been developed less; ②the majority of dosage forms are tablets, suppositories and other conventional dosage forms; ③there are few studies on the evaluation of vaginal mucosal preparations in vitro and in vivo. It is suggested that the future development of vaginal mucosal drug delivery system can be a useful attempt in the application of new technologies and methods, such as combination of drugs, high adhesion excipients, liposomes, etc;so as to provide reference for the application and improvement of vaginal mucosal drug delivery system.
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As a representative of controlled release preparations, osmotic pump has become a hot spot in the new preparation researches of Chinese materia medica (CMM). This paper reviewed CMM osmotic pump preparation from the following aspects: structure type of osmotic pump preparation, adjuncts of osmotic pump preparation of CMM, in vivo evaluation, and problems existing currently, which aimed to provide ideas and methods for the development of CMM osmotic pump preparation.
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We collected the data on the Sendeng-4 chemical composition corresponding targets through the literature and from DrugBank, SuperTarget, TTD (Therapeutic Targets Database) and other databases and the relevant signaling pathways from the KEGG (Kyoto Encyclopedia of Genes and Genomes) database and established models of the chemical composition-target network and chemical composition-target-disease network using Cytoscape software, the analysis indicated that the chemical composition had at least nine different types of targets that acted together to exert effects on the diseases, suggesting a "multi-component, multi-target" feature of the traditional Mongolian medicine. We also employed the rat model of rheumatoid arthritis induced by Collgen Type II to validate the key targets of the chemical components of Sendeng-4, and three of the key targets were validated through laboratory experiments, further confirming the anti-inflammatory effects of Sendeng-4. In all, this study predicted the active ingredients and targets of Sendeng-4, and explored its mechanism of action, which provided new strategies and methods for further research and development of Sendeng-4 and other traditional Mongolian medicines as well.
Subject(s)
Animals , Humans , Male , Rats , Anti-Inflammatory Agents , Chemistry , Arthritis, Rheumatoid , Drug Therapy , Genetics , Metabolism , Databases, Genetic , Drugs, Chinese Herbal , Chemistry , Gene Regulatory Networks , Medicine, Mongolian TraditionalABSTRACT
OBJECTIVE: To prepare and evaluate resveratrol-loaded mesoporous silica nanoparticles modified by amino (NH2-MSN-RES) to improve the bioavailability of resveratrol. METHODS: Mesoporous silica nanoparticles modified by amino (NH2-MSN) were synthesized by the modified Stober method. The structure of the nanoparticles were analyzed and characterized by FT-IR, Malvern particle size analyzer, and TEM. By introducing the innovative preparation process of repeated saturated solution adsorbing method, RES was encapsulated into NH2-MSN in larger amount. Dialysis bag method was used to investigate the in vitro drug release characteristics and MTT method was used to investigate the cytotoxicity on Caco-2 cells. The transport ability of the carrier was investigated by the Caco-2 cells monolayer model. Finally, the pharmacokinetics of NH2-MSN-RES was studied in rats. RESULTS: The particle size distribution of NH2-MSN was uniform with an average value of (98.4±2.8) nm, and the Zeta potential was (13.2±1.8) mv. Within the scope of 0-20 μg·mL-1, NH2-MSN had no obvious toxicity on Caco-2 cells. After 8 times of repeated adsorption, the drug loading of NH2-MSN-RES reached up to (19.26±2.51)%. In the drug release experiment, the cumulative release quantity of NH2-MSN-RES was 73.3% within 48 h, indicating sustained-release characteristics. NH2-MSN-RES had good ability of transmembrane transport in the Caco-2 cell monolayer model, and the two-way apparent permeability coefficient (Papp) was much larger than the RES solution. In the pharmacokinetic study, RES solution complied with one-compartment model, whereas NH2-MSN-RES complied with two-compartment model, indicating that the carrier changed the pharmacokinetic characteristics of RES. The AUC0-∞ of NH2-MSN-RES was 2.58-fold of that of RES solution, what's more, the t1/2, tmax, and ρmax of NH2-MSN-RES were significantly greater than those of RES solution. CONCLUSION: NH2-MSN is synthesized by modified Stober method successfully. Repeated saturated solution adsorbing method could effectively improve the drug loading. NH2-MSN-RES improves the bioavailability of RES prominently. NH2-MSN will be a promising nano-material for oral drug delivery carrier.
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OBJECTIVE: To evaluate the anti-hepatitis B virus (HBV) activity of herpetrione nanosuspension (PEDX-NS) both in vitro and in vivo. METHODS: HepG2 2.2.15 cells and duck hepatitis B virus (DHBV) infected ducks as in vitro and in vivo models were used to compare the anti-HBV activity of PEDX-NS and PEDX coarse suspension (PEDX-CS). RESULTS: In the HepG2 2.2.15 cell, PEDX-NS effectively suppressed the secretion of the HBV antigens (HBsAg and HBeAg) in a dose-dependent manner with significant difference from PEDX-CS (P<0.05 or P<0.01). In the in vivo evaluation, PEDX-NS with high dose (100 mg·kg-1) and middle dose (60 mg·kg-1) significantly reduced the serum HBV DNA level (P<0.05 or P<0.01) and the effect was better than that of PEDX-CS (P<0.05 or P<0.01). CONCLUSION: The result revealed that PEDX-NS exhibits anti-HBV activity both in vitro and in vivo and its effect was superior to that of PEDX-CS. The mechanism is probably that the small particle size of PEDX-NS provides a large specific surface area that resulted in better absorption in vivo, thus enhancing its anti-HBV activity.
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OBJECTIVE: To summary the common methods that used to assay dry powder inhaler in vivo, and provide a theoretical basis and some research ideas for relative research.
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Objective: To investigate the changes of matrine concentration in rat local skin with time after transdermal administration of matrine transfersomes, and to evaluate the transdermal delivery properties. Methods: The matrine transfersomes were applied non-occlusively onto rat skin in vivo with abdominal hair removal, and the concentration of drugs in microdialysate of skin was detected by microdialysis and reverse phase high performance liquid chromatography. Furthermore, the concentration-time curves of matrine in microdialysates of skin were compared among marine transfersomes, liposomes, and deoxysodium cholate solution. Results: After the transfersomes were given to rats, the maximum peak time (tmax) of matrine skin concentration appeared at (4.200 ± 0.447) h. The maximum skin concentration (Cmax) was (0.927 ± 0.251) μg/mL and area under the curve (AUC0-8) was (5.033 ± 1.526) μg·h·mL-1, which were much higher than those of the liposomes and the solution (containing 0.8% sodium deoxycholate, P < 0.05), while tmax shortened much more than that of them. Conclusion: In vivo skin microdialysis could be used to assess the transdermal delivery properties of matrine transfersomes. And matrine transfersomes have the good transdermal permeability and efficacy.