Optimization of rutaecarpine solid lipid nanoparticles by central composite design and response surface methodology / 中草药

Objective: To optimize the prescription of rutaecarpine solid lipid nanoparticles (Rut-SLN). Methods: Using the film-ultrasound method to lining-up the Rut-SLN, with the entrapment efficiency (EE), Zeta potential, and the average particle size as the evaluation indexes, using central composite design to inspect the effects of glycerol monostearate/drug quality ratio (A), soybean lecithin for injection/glycerol monostearate mass ratio (B), Poloxamer 188 (C) on three factors of the EE, Zeta potential, and average particle size. Prediction and analysis for selecting the best prescription condition were carried out by using the response surface method. Results: According to the optimized prescription, the EE, Zeta potential, and the average particle size of Rut-SLN was respectively 84.27%, 122.6 nm, and -20.7 mV. Conclusion: The optimal prescription of Rut-SLN has better stability, feasibility, and high EE, which is suitable for the production.

Preparation process of rutacarpine-hydroxypropyl-beta-cyclodextrin inclusion complex / 中国中药杂志

Rutaecarpine (Rut) is a type of indole quinazoline alkaloid exracted from Ruticarpum. Studies showed that Rut has a wide range of pharmacological effects, such as anti-hypertension, anticancer, anti-inflammation, anti-thrombus formation. Currently, many scholars are committed to developing it into a new antihypertensive and anti-inflammatory drug with all new mechanisms. But studies found that Rut is a highly fat-soluble drug with low water and oil solubility. Its high insolubility is the main obstacle in its oral absorption and application, which greatly reduced its bioavailability. Therefore, hydroxypropyl-beta-cyclodextrin (HP-beta-CD) was used as the inclusion material to prepare Rut-HP-beta-CD inclusion complex in this experiment, in order to increase its water solubility and bioavailability. In this experiment, the inclusion complex was prepared by the stirring-freeze-dry method. The preparation process was optimized by the orthogonal test, with the inclusion rate as the index, and molar ratio between host and guest molecules, inclusion temperature, time and stirring speed as the impacting factors. Moreover, the inclusion complex was verified by detecting the apparent solubility, thin layer chromatography, microscopic identification, melting point detection and dissolution study. The results showed that under the conditions of the molar ratio between Rut and HP-beta-CD of 1: 1, temperature at 60 degrees C, inclusion time of 4h and stirring speed at 600 r x min(-1), the inclusion rate of Rut-HP-beta-CD reached 91.04%. Therefore, the preparation process of Rut-HP-beta-CD inclusion under the optimum conditions is simple and feasible, with a highest inclusion rate and reproducibility, and could significantly improve Rut's solubility and bioavailability, and provide a reliable experimental basis for its clinical application.

Effect of photochemotherapy on expression of gelatases / 上海第二医科大学学报

Objective To determine the effect of photochemotherapy on the expression of gelatinases. Methods Reverse transcription-polymerase chain reaction and gelatine zymography were employed to detect the effect of photochemotherapy on the expression and bioactivity of gelatinases at mRNA and protein levels respectively. Results Combination of ultraviolet A(UVA,0.8-2.0 J/cm2) and 8-methoxypsoralen(8-MOP,100 ng/mL) resulted in a decrease in the expression and bioactivity of gelatinases. Conclusion Photochemotherapy can inhibit the angiogenesis of endothelial cells through downregulating the expression and bioactivity of gelatinases.

Cutaneous lesions and visceral involvement of tuberous sclerosis / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Tuberous sclerosis (TS) is an autosomal dominant disorder with a significant range of clinical expressions. The involvement of vital organs, such as the brain, kidney, heart and lung is the main cause of death in patients with TS. The aim of this study is to summarize the characteristic cutaneous features and common extracutaneous involvement of TS, which are helpful to the early detection of visceral involvement.</p><p><b>METHODS</b>The analyzed clinical data from 78 patients with TS included those from detailed history, physical and dermatological examination, cranial computed tomography (CT) and magnetic resonance imaging (MRI), abdominal ultrasonography, chest roentgenography, hand and foot X-ray and ophthalmologic examination.</p><p><b>RESULTS</b>The skin, brain and kidney were involved frequently in TS patients. Hypomelanotic macules were the most common and earliest cutaneous lesions. Their number was more than 3 in 81.5% of the patients. They were followed by facial angiofibromas and Shangreen's patch in a decreasing frequency. Forehead plaque, facial angiofibromas and Shagreen's patch appeared in patients at mean age of 2.6, 6.0 and 8.1 years respectively. Cranial CT showed a high positive rate in TS patients.</p><p><b>CONCLUSIONS</b>Cutaneous features of TS are helpful in the early diagnosis of the disease. Hypomelanotic macules are especially important for patients with epilepsy or babies whose number of hypomelanotic macules is more than 3. Cranial CT is of great value in the diagnosis of TS. The involvement of visceral organs such as the brain and kidney should be examined in TS patients.</p>