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To ascertain anti-fatigue constituents and mechanisms of Herpetospermum caudigerum.The 80% ethanol extracts of Herpetospermum caudigerum were partitioned with chloroform, ethyl acetate and n-butanol, respectively. Male Kunming mice were divided into 13 groups with 16 mice in each group: a control group fed with water, 9 groups treated with 3 fractions of Herpetospermum caudigerum (chloroform fraction, ethyl acetate fraction and n-butanol fraction) at dose of 80, 160 and 320 mg/kg for the low-dose group, medium-dose group and high-dose group, 3 herpetrione (HPE) treated groups fed with HPE at dose of 15, 30, and 60 mg/kg for the low-dose group, medium-dose group and high-dose group. All animals were treated once per day for 30 days. Anti-fatigue activity was assessed through the forced swimming test and serum biochemical parameters including blood lactic acid (BLA), blood urea nitrogen (BUN), malondialdehyde (MDA), hepatic glycogen (HG), lactic dehydrogenase (LDH), superoxide dismutase (SOD) and glutathione peroxidase (GPx) determined following the recommended procedures provided by the commercial kits.Compared with the control group, the lignans extract (ethyl acetate fraction) of Herpetospermum caudigerum and HPE could signifificantly prolonged the exhaustive swimming time (P0.05 or P0.01), and also increased the HG levels (P0.05 or P0.01) and the activities of antioxidant enzymes (SOD, GPx and LDH, P0.05 or P0.01); BLA and MDA levels were decreased considerably in lignans extract and HPE treated groups (P0.05 or P0.01). HPE also could significantly decrease the BUN contents compared with the control group (P0.05). The chloroform and n-butanol fraction showed no effect on swimming time and biochemical parameters.The lignans extract had antifatigue activities and HPE may be partly responsible for the anti-fatigue effects of Herpetospermum caudigerum. The possible mechanisms of anti-fatigue activity were related to the decrease of BUN and BLA, the increase of the HG storage and protecting corpuscular membrane by preventing lipid oxidation via modifying several enzyme activities.

The objective of this study was to prepare nanostructured lipid carrier (NLC)-based topical gel of Ganoderma Triterpenoids (GTs) and evaluate their effects on frostbite treatment. GT-NLCs was prepared by the high pressure homogenization method and then characterized by morphology and analyses of particle size, zeta potential, entrapment efficiency (EE), and drug loading (DL). The NLCs was suitably gelled for skin permeation studies in vitro and pharmacodynamic evaluation in vivo, compared with the GT emulgel. The GT-NLC remained within the colloidal range and was uniformly dispersed after suitably gelled by carbopol preparation. Transmission electron microscopy (TEM) study showed GT-NLCs was spherical in shape. The EE (%) and DL (%) could reach up to (81.84 ± 0.60)% and (2.13 ± 0.12)%, respectively. The result of X-ray diffractograms (XRD) showed that GTs were in an amorphous state in the NLC-gel. In vitro permeation studies through rat skin indicated that the amount of GTs permeated through skin of GT-NLCs after 24 h was higher than that of GT emulsion, and GT-NLCs increased the accumulative amounts of GTs in epidermis 7.76 times greater than GT emulsion. GT-NLC-gel was found to possess superior therapeutic effect for frostbite, compared with the GT emulgel. The NLC based topical gel of GTs could improve -their therapeutic effect for frostbite.

Qingyuan Lv,1 Xianyi Li,2 Baode Shen,1 He Xu,1 Chengying Shen,1 Ling Dai,1 Jinxia Bai,1 Hailong Yuan,1 Jin Han11Department of Pharmacy, 302 Military Hospital, 2Institute for Drug and Instrument Control, Health Department, General Logistics Department of People's Liberation Army, Beijing, People's Republic of ChinaAbstract: The aim of this study was to investigate the feasibility of using spray granulation as a drying method to convert phospholipid (PL)-sodium deoxycholate (SDC)-mixed micelles (MMs) containing a water-insoluble drug to a solid dosage form and to evaluate how drugs with significantly different physicochemical properties affect the spray granulation process and subsequent in vitro and in vivo processes. Cucurbitacin B (Cu B) and glycyrrhizin (GL) were used as the model drugs. After spray granulation, the dried Cu B-PL/SDC-MM powder was completely redispersible within 15 minutes in vitro. Meanwhile, the area under the curve during 24 hours (AUC0–24) and peak serum concentration from the dried powder were significantly (P

In this study, a novel orodispersible film (ODF) containing drug nanoparticles was developed with the goal of transforming drug nanosuspensions into a solid dosage form and enhancing oral bioavailability of drugs with poor water solubility. Nanosuspensions were prepared by high pressure homogenization and then transformed into ODF containing drug nanoparticles by mixing with hydroxypropyl methylcellulose solution containing microcrystalline cellulose, low substituted hydroxypropylcellulose and PEG-400 followed by film casting and drying. Herpetrione, a novel and potent antiviral agent with poor water solubility that extracted from Herpetospermum caudigerum, was chosen as a model drug and studied systematically. The uniformity of dosage units of the preparation was acceptable according to the criteria of Japanese Pharmacopoeia 15. The ODF was disintegrated in water within 30s with reconstituted nanosuspensions particle size of 280 ± 11 nm, which was similar to that of drug nanosuspensions, indicating a good redispersibility of the fast dissolving film. Result of X-ray diffraction showed that HPE in the ODF was in the amorphous state. In the in vitro dissolution test, the ODF containing HPE nanoparticles showed an increased dissolution velocity markedly. In the pharmacokinetics study in rats, compared to HPE coarse suspensions, the ODF containing HPE nanoparticles exhibited significant increase in AUC0-24h, Cmax and decrease in Tmax, MRT. The result revealed that the ODF containing drug nanoparticles may provide a potential opportunity in transforming drug nanosuspensions into a solid dosage form as well as enhancing the dissolution rate and oral bioavailability of poorly water-soluble drugs.

The purpose of this study was to design and optimize a novel drug nanoparticles-loaded oral fast dissolving film (NP-OFDF) using Box-Behnken design-response surface methodology.Drug nanosuspensions produced from high pressure homogenization were transformed into oral fast dissolving film containing drug nanoparticles by casting methods. Herpetrione (HPE), a novel and potent antiviral agent with poor water solubility that was extracted from Herpetospermum caudigerum, was studied as the model drug. The formulations of oral fast dissolving film containing HPE nanoparticles (HPE-NP-OFDF) were optimized by employing Box-Behnken design-response surface methodology and then systematically characterized.The optimized HPE-NP-OFDF was disintegrated in water within 20 s with reconstituted nanosuspensions particle size of 299.31 nm. Scanning electron microscopy (SEM) images showed that well-dispersed HPE nanoparticles with slight adhesion to each other were exposed on the surface of film or embedded in film. The X-ray diffractogram (XRD) analysis suggested that HPE in the HPE-NP-OFDF was in the amorphous state. In-vitro release study, approximate 77.23% of HPE was released from the HPE-NP-OFDF within 5 min, which was more than eight times compared with that of HPE raw materials (9.57%).The optimized HPE-NP-OFDF exhibits much faster drug release rates compared to HPE raw material, which indicated that this novel NP-OFDF may provide a potential opportunity for oral delivery of drugs with poor water solubility.

To observe in vitro the effect of rat drug serum on the proliferation of HSC-T6 hepatic stellate cells in the pharmacokinetic model for determining peoniflorin in Fufang Biejia Ruangan tablet, in order to discover the rational daily administration frequency of Fufang Biejia Ruangan tablet. Fufang Biejia Ruangan tablet was orally administered to rats with different daily administration frequency. Their blood was collected from veins behind eye sockets at different time points before the administration and after the first administration, in order to determine the concentration of peoniflorin in blood plasma and the effect of rat drug serums on the proliferation of HSC-T6. A comprehensive analysis was made on the relationship between pharmacodynamics and pharmacokinetics to determine the rational daily administration frequency of Fufang Biejia Ruangan tablet. The results showed a good correlation between the inhibitory effect of Fufang Biejia Ruangan tablet-contained serum on HSC-T6 and the concentration of peoniflorin in blood. The two-time administration group showed higher pharmacologic and pharmacokinetic AUCs than one-time administration and three-time administration groups. In conclusion, Fufang Biejia Ruangan table is recommended to be taken twice a day for treating liver fibrosis in chronic hepatitis.

In the present study, a novel hydrogel-grafted fabrics embedding of berberine nanosuspension was developed for the treatment of infected wound. Hydrogel-grafted fabric was prepared by graft copolymerization of N-isopropylacrylamide and alginate using ceric ammonium nitrate as initiator. Berberine nanosuspension was prepared and embedded in the hydrogel-grafted fabrics to achieve sustained drug release. The prepared hydrogel-grafted fabrics embedding of berberine nanosuspension was characterized by FT-IR spectroscopy, scanning electron microscopy, and swelling degree studies. Fourier transform infrared spectroscopy revealed that berberine was embedded into the matrix of hydrogel-grafted fabrics, rather than on the surface. Scanning electron microscopy showed that a thin hydrogel layer was formed on the surface of nonwoven fibers. The swelling study showed that hydrogel-grafted fabric had water absorbing characteristic with reversible temperature sensitivity. The drug release study demonstrated that hydrogel-grafted fabrics can be used as a sustained drug delivery system of hydrophobic compounds. The berberine nanosuspension embedded hydrogel-grafted fabric was further investigated in an animal infected wound model and was found to be a very promising wound healing dressing for the treatment and healing of infected wounds.

To prepare baicalin nanocrystal (BC-NC) and evaluate its pharmacokinetics in rats.Baicalin nanosuspensions (BC-NS) were prepared by the high pressure homogenization technology combined with ultrasonic, and then BC-NS were solidificated into BC-NC pellets by removing the water through fluid-bed drying. Its morphology, mean diameter and Zeta-potential were determined. An HPLC method was employed to determine the concentration of baicalin in plasma, and the bioavailability of the nanocrystal was compared with the reference group by oral administration in Wistar rats.The nanocrystals observed by scanning electron microscopy were irregular granulated, and the mean particle sizes of BC-NC were (248 +/- 6) nm. Its polydispersity index (PI) and zeta-potential were (0.181 +/- 0.065), (-32.3 +/- 1.8) mV, respectively. The pharmacokinetic parameters showed that the C(max) was (16.54 +/- 1.73) mg x L(-1) and the AUC(0-24 h) was (206.96 +/- 21.23) mg x L(-1) x h, which were significantly enhanced compared with the baicalin bulk and baicalin physical mixture (BC-PM) formulation, respectively (P0.01).Baicalin nanocrystal can significantly improve the bioavailability of baicalin.