Progress of nanopreparation technology applied to volatile oil drug delivery systems.

Traditional Chinese medicine volatile oil has a long history and possesses extensive pharmacological activity. However, volatile oils have characteristics such as strong volatility, poor water solubility, low bioavailability, and poor targeting, which limit their application. The use of volatile oil nano drug delivery systems can effectively improve the drawbacks of volatile oils, enhance their bioavailability and chemical stability, and reduce their volatility and toxicity. This article first introduces the limitations of the components of traditional Chinese medicine volatile oils, discusses the main classifications and latest developments of volatile oil nano formulations, and briefly describes the preparation methods of traditional Chinese medicine volatile oil nano formulations. Secondly, the limitations of nano formulation technology are discussed, along with future challenges and prospects. A deeper understanding of the role of nanotechnology in traditional Chinese medicine volatile oils will contribute to the modernization of volatile oils and broaden their application value.

Transcriptomic changes in the hypothalamus of ovariectomized mice: Data from RNA-seq analysis.

BACKGROUND: Menopausal symptoms can affect the physical and mental health of females and are often related to abnormal function of the hypothalamus. In this study, we evaluated changes in the hypothalamus transcriptome in ovariectomized mice to identify key mRNAs, and systematically elucidated the possible molecular mechanisms underlying the menopausal syndrome to provide a theoretical basis for clinical diagnosis and treatment. METHODS: Forty-six adult female C57BL/6 J mice were randomly divided into SHAM and OVX groups, 23 mice per group. Eight weeks after the procedure, differentially expressed genes (DEGs) in the hypothalamus were identified through RNA-sequencing. DEGs were analyzed using Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genome (KEGG) analyses. Key DEGs were then evaluated using quantitative reverse transcription-polymerase chain reaction (qRT-PCR) and immunohistochemical staining. RESULTS: Compared with SHAM group, 7295 genes were upregulated, and 8979 genes were downregulated in the hypothalamus of OVX mice with a fold change of 1.5 (log2 fold change ≥0.585). GO and KEGG analyses suggested these key genes were involved in thermoregulation, food intake, glucose and lipid metabolism, cardiovascular regulation, biological rhythm, and endocrine regulation. CONCLUSIONS: Differential expression of genes in the hypothalamus of OVX mice involved in thermoregulation, eating, sleeping, homeostasis, and endocrine regulation 8 weeks after ovariectomy suggest potential roles in the pathogenesis of climacteric syndrome.

Effect of Huang-Lian Jie-Du Decoction on Glucose and Lipid Metabolism in Type 2 Diabetes Mellitus: A Systematic Review and Meta-Analysis.

Background: Type 2 diabetes mellitus (T2DM) is a heterogeneous disease characterized by persistent hyperglycemia. Huang-Lian Jie-Du decoction (HLJDD) is a traditional Chinese medicine formula which is widely used in treating T2DM in China. A thorough understanding of current body of evidence is needed. Objective: this study aims to summarize the clinical evidence of HLJDD for T2DM to provide an up-to-date and accurate understanding of this issue for research and clinical practice. Methods: Six databases were searched from inception to June 27, 2020 without language and publication status restrictions and randomized controlled trials about HLJDD on T2DM were included. Two evaluators searched and screened citations independently. Risk of bias was assessed by 2019 version 2 of the Cochrane risk-of-bias tool for randomized trials (RoB2). Risk ratio (RR) with 95% confidence interval (CI) was used as an effect measure for dichotomous outcomes and mean difference (MD) with 95% CI was used for continuous outcomes. Subgroup analyses and sensitivity analyses were carried out. Results: Nine studies including 811 participants were included in this study. The overall risk of bias was high risk. Compared with metformin alone, combination treatment of HLJDD and metformin may result in a reduction in HbA1c, FBG, 2hPG, HOMA-IR and an improved lipid metabolism. Evidence comparing HLJDD and metformin or no intervention or placebo was insufficient. The quality of evidence was low. Conclusions: Current evidence about HLJDD on T2DM is still uncertain and more high-quality studies are needed to firmly establish the clinical efficacy and safety of HLJJD.

Baicalin Liposome Alleviates Lipopolysaccharide-Induced Acute Lung Injury in Mice via Inhibiting TLR4/JNK/ERK/NF-κB Pathway.

Acute lung injury (ALI) and acute respiratory distress syndrome (ARDS) are challenging diseases with the high mortality in a clinical setting. Baicalin (BA) is the main effective constituent isolated from the Chinese medical herb Scutellaria baicalensis Georgi, and studies have proved that it has a protective effect on ALI induced by lipopolysaccharide (LPS) due to the anti-inflammatory efficacy. However, BA has low solubility which may limit its clinical application. Hence, we prepared a novel drug delivery system-Baicalin liposome (BA-LP) in previous research-which can improve some physical properties of BA. Therefore, we aimed to explore the effect of BA-LP on ALI mice induced by LPS. In pharmacokinetics study, the values of t 1/2 and AUC0- t in the BA-LP group were significantly higher than that of the BA group in normal mice, indicating that BA-LP could prolong the duration time in vivo of BA. The BA-LP group also showed a higher concentration in lung tissues than the BA group. Pharmacodynamics studies showed that BA-LP had a better effect than the BA group at the same dosage on reducing the W/D ratio, alleviating the lung injury score, and decreasing the proinflammatory factors (TNF-α, IL-1ß) and total proteins in bronchoalveolar lavage fluids (BALF). In addition, the therapeutic effects of BA-LP showed a dose-dependent manner. Western blot analysis indicated that the anti-inflammatory action of BA could be attributed to the inhibition of the TLR4-NFκBp65 and JNK-ERK signaling pathways. These results suggest that BA-LP could be a valuable therapeutic candidate in the treatment of ALI.

Nose to brain drug delivery - A promising strategy for active components from herbal medicine for treating cerebral ischemia reperfusion.

Cerebral ischemia reperfusion injury (CIRI), one of the major causes of death from stroke in the world, not only causes tremendous damage to human health, but also brings heavy economic burden to society. Current available treatments for CIRI, including mechanical therapies and drug therapies, are often accompanied by significant side-effects. Therefore, it is necessary to discovery new strategies for treating CIRI. Many studies have confirmed that the herbal medicine has the advantages of abundant resources, good curative effect and little side effects, which can be used as potential drug for treatment of CIRI through multiple targets. It's known that oral administration commonly has low bioavailability, and injection administration is inconvenient and unsafe. Many drugs can't delivery to brain through routine pathways due to the blood-brain-barrier (BBB). Interestingly, increasing evidences have suggested the nasal administration is a potential direct route to transport drug into brain avoiding the BBB and has the characteristics of high bioavailability for treating brain diseases. Therefore, intranasal administration can be treated as an alternative way to treat brain diseases. In the present review, effective methods to treat CIRI by using active ingredients derived from herbal medicine through nose to brain drug delivery (NBDD) are updated and discussed, and some related pharmacological mechanisms have also been emphasized. Our present study would be beneficial for the further drug development of natural agents from herbal medicines via NBDD.

Pharmacokinetics, pharmacodynamics and toxicity of Baicalin liposome on cerebral ischemia reperfusion injury rats via intranasal administration.

Baicalin (BA) is a major active component from the traditional Chinese medicine, which has been widely used to treat brain diseases. Previously, the baicalin liposome (BA-LP) was prepared to improve its low bioavailability. However, the existence of the obstacles such as the blood-brian-barrier (BBB) still make it difficult to enter brain effectively. Meanwhile, many reports have shown that drugs can be transported into brain through intranasal administration without the BBB. Therefore, we aim to explore the effect of BA-LP on middle cerebral artery occlusion (MCAO) rats via i.n. administration. The results showed that BA and BA-LP had no obvious impact on mucosa after i.n. administration. And in pharmacokinetics study after i.n. administration, the value of t 1/2 and AUC 0-t in BA-LP group were significantly higher than that of the BA group (p < 0.05), indicating BA-LP could prolong the extension time of BA in vivo and further improve the bioavailability. In the brain biodistribution, the BA-LP group showed a higher BA concentration in brain tissues. Pharmacodynamics studies showed that BA-LP through i.n. administration could significantly improve the neurological deficits, cerebral infarction and brain pathological status in rats with MCAO surgery. Obviously, the BA-LP was more effective after nasal administration than intravenous administration, suggesting the nasal administration is more advantageous route in brain concentration enrichment. In conclusion, BA-LP could be safely used in i.n. administration, which can effectively improve brain targeting effect and thus protect the MCAO rats. Furthermore, successful use of the BA-LP via nasal delivery can provide a model for other drugs with neuroprotective effect and further promote the cure rate of brain diseases.