Latest ArticlesNanocrystals possess the merits of high solubility, fast dissolution rate and high bioavailability with extremely small particle size, so they have been used in various formulations for oral, injectable, transdermal or mucosal delivery. Although injectable drug delivery is relatively reliable, the transport process of nanocrystals after injection is more complicated than that of solution. Based on literature research, this paper reviews the mechanisms of absorption, distribution, metabolism and excretion of injectable nanocrystals. Meanwhile, it also describes the factors affecting their processes in vivo, including the influence of physiological factors such as injection site, mononuclear phagocyte system, and formulation factors such as drug particle size and stabilizer. All of these provide a good foundation for further extensive application.
Ionic liquids (ILs) are a class of salts that appear liquid form at or near room temperature. They are widely used in biomedicine, especially in transdermal drug delivery, because of their simple preparation process, high stability, good solubility and flexible structure. ILs can improve drug solubility, promote transdermal penetration, improve the efficacy of drugs, and solve the problems existing in the transdermal drug delivery. This article reviewed the classification, synthesis methods and its application in transdermal drug delivery. The IL-based transdermal preparation was also summarized, in order to provide reference for further research and development of ILs in transdermal drug delivery.
Targeted protein degradation (TPD) strategies have been used by academia and industry as one of the promising new drug development technologies to address targeted proteins that are not effectively acted upon by conventional small molecule inhibitors. Protein hydrolysis-targeted chimeras (PROTAC) have become the most well-studied protein-targeted degradation technique in TPD, which comprises of a POI-binding ligand, an E3 ligand, and a linker connecting the two ligands. Once the POI ligand binds to the receptor protein, PROTAC recruits the E3 ligand to ubiquitinate the protein and finally degrades it through the ubiquitin-proteasome system. PROTAC technology offers great potential for therapeutic applications because it can target proteins that lack well-defined active degradation sites, which are often involved in the pathogenesis of cancer and other diseases. To enhance PROTAC's target delivery and tissue selectivity, the industry has begun to investigate new strategies, such as discovering new E3 ligases and developing corresponding ligands, along with continuing to investigate more emerging PROTAC modalities to further promote PROTAC. These strategies and relevant studies are discussed in this review.
To evaluate the clinical safety and effectiveness of Jiuwei Zhike mixture in the treatment of wind-heat cough syndrome of acute bronchitis.
A randomized, double-blind, double-simulation, placebo and positive drug controlled, multi-center clinical trial design was adopted. The selected disease was acute bronchitis (wind-heat cough syndrome). Seven hundred subjects from 10 research centers were planned to be included and divided into treatment group, positive drug control group and placebo group in a ratio of 3∶1∶1. The patients took Jiuwei Zhike mixture+Jizhi syrup simulation agent, Jiuwei Zhike mixture simulation agent+Jizhi syrup, or Jiuwei Zhike mixture simulation agent+Jizhi syrup simulation agent for 7 d.
Jiuwei Zhike mixture took effect on acute bronchitis (wind-heat cough syndrome) from the 3rd day of administration. By the 7th day of administration, 54.7% of the subjects' cough symptoms completely disappeared (49.2% in the positive drug group and 15.1% in the placebo group), with a clinical recovery rate of about 51.6% (43.5% in the positive drug group and 13.7% in the placebo group), and a total effective rate of 93.4% (87.1% in the positive drug group and 41.9% in the placebo group). And it had a significant improvement effect on the symptoms of the disease.
Jiuwei Zhike mixture is safe and effective in treating acute bronchitis (wind-heat cough syndrome) and its curative effect is not inferior to Jizhi syrup and superior to placebo.
To optimize the water extraction process of modified Tabusen-2 by response surface methodology (Box-Behnken) and investigate its in vitro efficacy.
Taking the mass fractions of caffeic acid and geniposide as the comprehensive score, response surface methodology was used to optimize the soaking time, material-to-liquid ratio, extraction time and extraction times. The RAW 264.7 cells induced by nuclear factor-κB receptor activator ligand (RANKL) were co-cultured with the optimal extracts for 5 d, and then treated with tartrate-resistant acid phosphatase (TRAP). The TRAP-positive cells were stained and observed under a microscope to evaluate the in vitro efficacy of the extract.
The extraction time, soaking time, and material-to-liquid ratio were selected as the inspection factors, and the comprehensive score of caffeic acid and geniposide content was used as the evaluation index. After optimization by response surface method, the optimal extraction condition was 540 min; the liquid ratio was 1∶12 (g·mL-1); the extraction time was 44 min, and the extraction times were two times. The extract obtained under this condition had a significant inhibitory effect on RAW264.7 cells induced by RANKL, could reduce TRAP-positive cells, and inhibited multinucleation.
The water extraction process of modified Tabusen-2 optimized by response surface analysis method is reproducible, stable and feasible, and has good in vitro pharmacodynamic activity, laying a reliable foundation for future in vivo pharmacodynamic experimental research.
To optimize the preparation and solidification process of paeonol nanosuspensions.
Paeonol nanosuspensions was prepared by solvate-non-solvent precipitation method. With the appearance character, particle size and polymer dispersity index (PDI) as the evaluation indexes, the type of stabilizer, stirring time, stirring speed, drug-auxiliary ratio, organic phase-water ratio and water phase temperature as the influencing factors, the preparation process of nanosuspensions was optimized, and the stability of the prepared nanosuspensions was investigated. The freeze-drying method was used for solidification, and the effect of freeze-drying protectant on solidification was investigated. The drug loading, scanning electron microscopy, differential scanning calorimetry, X-ray diffraction and dissolution in vitro of the solidified nanosuspensions were characterized.
The preparation process of paeonol nanosuspensions was povidone K60 as stabilizer, drug-to-auxiliary ratio 1∶3, organic phase water ratio 1∶10, at 25 ℃, 400 r·min-1 magnetic stirring for 30 min. The prepared nanosuspensions had a particle size of about 40 nm, with narrow distribution and good stability. The lyophilized protectant was determined to be 5% trehalose. The drug loading capacity of solidified nanosuspensions was 21.63%, and the microscopic surface morphology was spherical, and the drug structure changed from crystalline form to amorphous form. The cumulative dissolution rate of the suspension reached 87.12% in 1 h.
The formulation and preparation process of paeonol nanosuspensions are simple, easy to operate, with good formability after solidification and fast dissolution, which lay a foundation for the development of more dosage forms.
To explore the effect and mechanism of compound cortex phellodendri fluid in bacterial vaginosis rats via TLR4/NF-κB pathway.
Fifty-five SD female rats were selected to construct bacterial vaginosis model by injection of mixed bacterial liquid. After successful modeling, the rats were treated with compound cortex phellodendri fluid, metronidazole vaginal gel, and Honghe fujie lotion, respectively. After 7 d of continuous treatment, inflammatory cell infiltration and glycogen accumulation in rat vaginal tissues were observed by HE staining. ELISA method was used to detect the expression level of IL-1β, IL-2, IL-10, IL-6, and TNF-α in the vaginal lavage. The distribution of NF-κB p65 in rat vaginal tissues were located by immunohistochemical method. And the protein expression level of TLR4 and NF-κB p65 were detected by Western blot.
Compared with those of the model group, the infiltration of inflammatory cells in compound cortex phellodendri fluid group was reduced, and the accumulation of glycogen was significantly increased (P<0.01), the concentrations of IL-1β (P<0.01), IL-6 (P<0.05), IL-2, and TNF-α in the vaginal lavage were decreased, while the IL-10 concentration increased (P>0.05), the protein expression level of TLR4 and NF-κB p65 decreased (P<0.05), and the NF-κB p65's translocated nuclear were suppressed (P<0.01).
Compound cortex phellodendri fluid has a definite therapeutic effect on bacterial vaginosis rats. Its mechanism may be related to the inhibition of TLR4/NF-κB pathway and adjustion of immune imbalance on Th1/Th2.
This article reviewed the reports of adverse reactions of 17 weight-loss drugs approved by the FDA since 1887 during the clinical trials and after their marketing, including six that are still on the market and 11 that have been withdrawn due to valvular heart disease, suicidal tendencies, cancer risk, or other reasons. Weight-loss drugs can reduce weight and bring metabolic benefits in obese patients, but also cause various side effects, including psychonervous system adverse reactions, cancer risk, cardiotoxicity, liver damage, pancreatic toxicity, renal toxicity, digestive tract side effects, etc. Drugs with severe side effects will receive a black box warning from the FDA, and drugs with fatal side effects will be ordered to withdraw from the market. In addition to summarizing the side effects of weight-loss drugs, this article put forward some in-depth considerations on their safety, in order to provide reference for pharmaceutical companies to develop weight-loss drugs, clinicians and patients to use weight-loss drugs correctly and protect people's lives and health.
During the past ten years, the research and development of new drugs for skin diseases have boomed. The new drugs including biologics and small molecules have rapidly developed and greatly improved the treatment of common inflammatory/immunological skin diseases. More than 200 clinical trials have been performed and many new drugs was approved in China, bringing the dermatological treatment to a new era. In this paper, recent progress was reviewed in new drug development on psoriasis, atopic dermatitis, alopecia areata and androgenetic alopecia in China.
Since the reform of the drug review and approval system, with the support of a series of policies and technology that encourages innovation, a large number of clinical trial application of new drugs for skin disease has been approved. In addition, innovative drugs, high-quality generic drugs, and biosimilar products have been accelerately approved, which meets the availability and accessibility of drugs to a certain extent. In order to guide innovation and scientific development of new drugs for skin disease, this article reviews the reform of drug review and approval system, the continuous improvement of the drug regulatory system, and the progress in development, evaluation and approval of new drugs for skin disease in China. We focus on the challenges, opportunities, and improvement measures faced in the development, evaluation, and regulation of drugs in this field. With multiple measures simultaneously taken, the goal is to meet the urgent clinical medication needs of patients with skin disease, so that effective and safe drugs can benefit patients as soon as possible.
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