A Non-Lipolysis Nanoemulsion Improved Oral Bioavailability by Reducing the First-Pass Metabolism of Raloxifene, and Related Absorption Mechanisms Being Studied.

Objective: A non-lipolysis nanoemulsion (NNE) was designed to reduce the first-pass metabolism of raloxifene (RAL) by intestinal UDP-glucuronosyltransferases (UGTs) for increasing the oral absorption of RAL, coupled with in vitro and in vivo studies.

Methods: In vitro stability of NNE was evaluated by lipolysis and the UGT metabolism system. The oral bioavailability of NNE was studied in rats and pigs.

Nanoemulsion improves hypoglycemic efficacy of berberine by overcoming its gastrointestinal challenge.

Berberine (BBR) is an important natural product with poor gastrointestinal behavior includes low permeability, P-glycoprotein efflux, and mass elimination in the intestine. The aim of this study was to develop a novel nanoemulsion (NE) to improve the hypoglycemic efficacy of BBR. NE was prepared and characterized by morphology and droplet size detection, stored stability, in vitro intestinal lipolysis and metabolism, Caco-2 cells transport, in situ single-pass intestinal perfusion, oral bioavailability in rats, and hypoglycemic efficacy in high-fat diet and streptozocin-induced mice.

Research progress on berberine with a special focus on its oral bioavailability.

The natural product berberine (BBR) has become a potential drug in the treatment of diabetes, hyperlipidemia, and cancer. However, the oral delivery of BBR is challenged by its poor bioavailability. It is necessary to improve the oral bioavailability of BBR before it can be used in many clinical applications.

[Preparation and Dissolution Evaluation of Breviscapine Self-microemulsion].

Objective: To study the prescription and preparation technology of breviscapine self-microemulsion for oral administration, and to evaluate the quality, stability and in vitro dissolution.

Methods: The prescription and preparation technology were selected and optimized through the solubility experiment, compatibility test, and pseudo-ternary phase diagram method, using the self-emulsifying time, appearance, particle diameter and stability as indexes. The droplet morphous, drug content, stability and dissolution were evaluated.

[Preparation and quality evaluation of tanshinone IIA microemulsion for parenteral injection].

Objective: To study the prescription and preparation technology of tanshinone IIA microemulsion for parenteral injection, and to evaluate its quality.

Methods: The prescription was selected and optimized through single-factor test, compatibility experiment and the pseudo-ternary phase diagram method. The preparation technology was investigated, and the droplet morphous, particle diameter, zeta potential, stability and haemolyticus were evaluated.

Lobelia chinensis: chemical constituents and anticancer activity perspective.

Research has demonstrated that many chemical constituents dominated by piperidine alkaloids and flavonoids, such as lobelanidine, lobeline, and lobelanine, have been obtained from Lobelia chinensis Lour. Experimental studies and clinical applications have also indicated that L. chinensis possesses a number of pharmacological activities (e.

[Drug delivery systems of baicalin, baicalin-phospholipid complex and self-microemulsifying drug across Caco-2 cell model].

Objective: To study the absorption of baicalin (BA), baicalin-phospholipid complex (BA-PC), and two kinds of self-microemulsifying drug delivery system (SMEDDS) of BA-PC (BA-PC-NE-SMEDDS with natural emulsifier and BA-PC-NS-SMEDDS with nonionic surfactants) and predict the ability of improving bioavailability through changing the formulation of BA.

Methods: Transmembrane transports of each formulation were studied by Caco-2 cell model and the concentration of BA was determined by HPLC.

Results: With the increasing concentration of BA, the transport rate and apparent permeability coefficient (Papp) of BA was increased,indicating the passive absorption mechanism of BA.

The pharmacokinetics of recombinant human interferon-alpha-2b poly(lactic-co-glycolic acid) microspheres in rats.

Interferon-alpha2b (IFN α-2b) microspheres were prepared at various concentrations (5%, 10%, 15%, 20% and 25%) and viscosities (0.39, 0.6, 0.

[Preparation and in vitro evaluations of topically applied capsaicin transfersomes].

Objective: Capsaicin transfersomes were prepared and its quality specifications were evaluated.

Method: Capsaicin transfersomes were prepared by high shear dispersing machine and evaluated on the entrapment efficiency, drugs release rate and in vitro skin permeation.

Result: Capsaicin transfersomes is composed of single unilamellar vesicles, with average size of 150.

[Determination of capsaicin in Pheretima aspergillum from different habitats by RP-HPLC].

Objective: To determine the content of hypoxanthine in Pheretima aspergillum from different habitats.

Method: A RP-HPLC method was established. The chromatographic column was Inertsil ODS-EP.

[Preparation and in vitro and in vivo evaluations of topically applied capsaicin transfersomes].

Aim: To prepare capsaicin transfersomes and evaluate them in vitro and in vivo.

Methods: Capsaicin transfersomes were prepared by high shear dispersing machine and evaluated by entrapment efficiency, release rate, in vitro skin permeation and distribution in different tissues in vivo.

Results: Capsaicin transfersomes were composed of single unilamellar vesicles with an average diameter of 150.

[The preparation and the in vitro release of OANO-1 microspheres].

Objective: To prepare OANO-1 microspheres and test their release in vitro.

Method: OANO-1 microspheres were made by W/O/W-liquid drying process. The surface morphology of the microspheres was observed by SEM.