Preparation of Rubra (Paeonia lactiflora Pall.) extract and studies in activity and skin penetration.

The inhibition rate of tyrosinase activity was used to determine extraction solvent of Paeoniae Radix Rubra extract (PRRE), which was established quality control standards by HPLC and verified the antioxidant activity. Ternary phase diagram was used to screen the best formulation of PRRE nanoemulsion, the skin permeability of PRRE and nanoemulsion were compared. The results show that 70% ethanol as the extraction solvent were highest (88.

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.

Comparisons of in vitro Fick's first law, lipolysis, and in vivo rat models for oral absorption on BCS II drugs in SNEDDS.

Purpose: The objective of this study was to compare the in vitro Fick's first law, in vitro lipolysis, and in vivo rat assays for oral absorption of Biopharmaceutical Classification Systems Class II (BCS II) drugs in self-nanoemulsifying drug delivery system (SNEDDS), and studied drugs and oils properties effects on the absorption.

Methods: The transport abilities of griseofulvin (GRI), phenytoin (PHE), indomethacin (IND), and ketoprofen (KET) in saturated water solutions and SNEDDS were investigated using the in vitro Madin-Darby canine kidney cell model. GRI and cinnarizine (CIN) in medium-chain triglycerides (MCT)-SNEDDS and long-chain triglycerides (LCT)-SNEDDS were administered in the in vivo SD rat and in vitro lipolysis models to compare the oral absorption and the distribution behaviors in GIT and build an in vitro-in vivo correlation (IVIVC).

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.

Niosomal Nanocarriers for Enhanced Skin Delivery of Quercetin with Functions of Anti-Tyrosinase and Antioxidant.

This study aimed to screen an effective flavonoid with promising whitening and antioxidant capacities, and design flavonoid-loaded niosomes to improve its solubility, stability, and penetration. In vitro anti-tyrosinase and 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging experiments were conducted to investigate the whitening and antioxidant capacities of several flavonoids, including quercetin, morin, festin, myricetin, rutin, and breviscapine. The conductivity, viscosity, and particle size of Span60-RH40-based formulation of nonionic surfactant vesicles (niosomes) with different mass ratios were studied to determine the most appropriate formulation.

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.

Evaluation of the anaphylactoid potential of Andrographis paniculata extracts using the popliteal lymph node assay and P815 cell degranulation in vitro.

Background: The anaphylactoid reactions induced by andrographis injection have repeatedly been reported. The aim of our study was to evaluate the immuno-sensitizing potential of extracts from Andrographis paniculata Nees and to screen for the constituent that is responsible for inducing the anaphylactoid reaction.

Methods: In the direct popliteal lymph node assay (D-PLNA), female BALB/c mice were randomly divided into several groups with ten mice per group according to the experiment design, the right hind footpads of mice received a single subcutaneous injection of Andrographis paniculata (50 μl), and the left hind footpads received the same volume of vehicle.

Combined use of phospholipid complexes and self-emulsifying microemulsions for improving the oral absorption of a BCS class IV compound, baicalin.

The aim of this study was to develop a formulation to improve the oral absorption of baicalin (BA) by combining a phospholipid complex (PC) and self-emulsifying microemulsion drug delivery system (SMEDDS), termed BA-PC-SMEDDS. BA-PC was prepared by a solvent evaporation method and evaluated by complexation percentage (CP). The physicochemical properties of BA-PC were determined.

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.

Formulation and characterization of Brucea javanica oil microemulsion for improving safety.

Objective: This study engaged in investigation of optimal formulation, characteristics analysis of Brucea javanica oil microemulsion (BJOM) in order to address safety concerns and make recommendations for improvements in BJOM safety during clinical use in vivo.

Methods: Pseudo-ternary phase diagram techniques were used to determine the appropriate ratio of surfactant, cosurfactant and oil phases. Subsequent stability testing of BJOM was performed by dilution, centrifugation and accelerated stability testing.

[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.