Baicalein-modified chitosan nanofiber membranes with antioxidant and antibacterial activities for chronic wound healing.

Diabetic foot ulcers, burns and many other trauma can lead to the formation of skin wounds, which often remain open for a long period of time, seriously affecting the quality of patient's life. Oxidative stress and infection are the main factors affecting the healing of chronic wounds, so it is important to develop dressings with dual antioxidant and antimicrobial properties for wound management. In this study, functionalized chitosan was synthesized by modifying chitosan with antioxidant baicalein to enhance the antimicrobial and antioxidant activities of chitosan. Then the obtained baicalein-modified chitosan was prepared into nanofibrous membranes by electrospinning. The membrane structures were characterized, and the antioxidant and antibacterial activities were evaluated by in vivo and in vitro experiments. The results showed that the prepared wound dressings had excellent antioxidant and antibacterial activities and significantly accelerated the wound process. This study provided a reference for the development of novel dressing materials to promote wound healing.

HPLC combined with chemometrics for quality control of Huamoyan Granules or Capsules.

Objective: Huamaoyan Granules (HMYG) and Huamaoyan Capsules (HMYC) are Chinese patent medicines with different dosage forms of the same prescription. Due to the different preparation process, the chemical composition of these Chinese patent medicines varies greatly among different forms, but there were few studies on the difference comparison and quality control of them. In order to improve the effectiveness and safety in its clinical application, an idea combining high performance liquid chromatography (HPLC) and chemometrics was put forward to study the quality control of Chinese patent medicines in different dosage forms of the same prescription. Methods: The differential markers of HMYG and HMYC were explored based on HPLC fingerprint and chemometrics including orthogonal projections to latent structures-discriminant analysis (OPLS-DA), principal component analysis (PCA), and hierarchical cluster analysis (HCA). Finally, the quantitative analysis method of related components was established by HPLC. Results: A quality control method for HMYG and HMYC was established. Firstly, the chemical components of HMYG and HMYC were systematically analyzed by HPLC fingerprinting. Further exploration showed that there were 20 characteristic peaks and 57 common peaks. Then, the potential differential markers between HMYG and HMYC were explored by chemometrics, and the differential markers were screened after intersection with the 20 characteristic peaks. Finally, HPLC quantitative analysis methods for nine components were established, including seven differential markers (neochlorogenic acid, protocatechualdehyde, chlorogenic acid, cryptochlorogenic acid, caffeic acid, rosmarinic acid and salvianolic acid A). The results of HPLC quantitative analysis showed that the contents of eight components in HMYG and HMYC samples were significantly different. According to the above results, the differential markers between HMYG and HMYC screened based on HPLC fingerprint and chemometrics can effectively characterize the differences between the two dosage forms. Conclusion: The present work provides a rapid and effective method for routine quality evaluation and control of HMYG and HMYC. This work also provides feasible methods for the quality evaluation and control of Chinese patent medicines with different dosage forms of the same prescription.

[Optimization of extraction process for classic prescription Yihuang Decoction based on Box-Behnken design-response surface methodology, standard relation, and analytic hierarchy process combined with entropy weight method].

Based on the concept of quality by design(QbD), the Box-Behnken design-response surface methodology combined with standard relation(SR) and analytic hierarchy process(AHP)-entropy weight method(EWM) was applied to optimize the extraction process of the classic prescription Yihuang Decoction. The content of geniposidic acid, phellodendrine hydrochloride, and berberine hydrochloride in Yihuang Decoction, the extract yield, and fingerprint similarity were used as the critical quality attributes(CQAs) of the extraction process. The extraction time, water addition, and extraction times were used as the critical process parameters(CPPs). After determining the levels of each factor and level through single-factor experiments, response surface experiments were designed according to the Box-Behnken principle, and the experimental results were analyzed. The SR between each sample and the reference sample under various evaluation indicators of different extraction parameters was calculated. The weights of the five evaluation indicators were determined using AHP-EWM, followed by comprehensive evaluation. A function model between CPPs and CQAs characterized by comprehensive scores was established to predict the optimal extraction process parameters. In the final comprehensive weight coefficients, the yield rate accounted for 43.1%, and the content of berberine hydrochloride, phellodendrine hydrochloride, and geniposidic acid accounted for 35.1%, 6.3%, and 15.5%, respectively. After comprehensive score analysis with SR, the established second-order polynomial model was statistically significant(P<0.01, and the lack of fit was not significant). The predicted optimal extraction conditions for Yihuang Decoction were determined as follows: 8-fold volume of water, extraction time of 1.5 h, and extraction once. The mean comprehensive score of the validation experiment was 85.77, with an RSD of 0.99%, and it met the quality control stan-dards for the reference sample of Yihuang Decoction. The results indicate that the optimized extraction process for Yihuang Decoction is stable and reliable, and the water extract is close in quality attributes to the reference sample. This can serve as a foundation for the research and development of granules in the future. Box-Behnken design-response surface methodology combined with SR and AHP-EWM can provide references for the modern extraction process research of other classic prescriptions.

Study of the permeation-promoting effect and mechanism of solid microneedles on different properties of drugs.

In transdermal drug delivery systems, the physicochemical properties of the drug affect its percutaneous permeability. However, whether the physicochemical properties of drugs change their transdermal permeability in the presence of pores in the presence of solid microneedles (MNs) has been less studied in this area. In this project, cinnamaldehyde, curcumin, ferulic acid and geniposide were selected as model drugs for the study of their transdermal permeability under the action of MNs, and a combination of classical experiments and visualization means such as scanning electron microscopy and laser confocal was used to investigate the permeation-promoting mechanism of MNs. The results showed that the MNs had significant permeation-promoting effects on different properties of drugs, with the permeation-promoting effects on cinnamaldehyde, curcumin, ferulic acid and geniposide being 6.36, 17.43, 29.54 and 8.91 times, respectively, and the permeation-promoting effects were more pronounced for lipid-soluble and amphiphilic drugs. Using scanning electron microscopy, transmission electron microscopy and other means to confirm that MNs can promote the penetration by acting on the skin to produce pores, and their effect on skin structure is greater than that of drugs. In addition, the existence of pores increases the amount of drug transdermal, which may enhance the diffusion of drug on the skin, and has no effect on lipid exchange and transdermal route. Through the research, it has been found that MNs is equivalent to direct peeling of the stratum corneum (SC), but it is simpler and safer for the patient.

Anti-neuroinflammatory effects of dimethylaminomylide (DMAMCL, i.e., ACT001) are associated with attenuating the NLRP3 inflammasome in MPTP-induced Parkinson disease in mice.

Parthenolide (PTL) is a natural compound with anti-inflammatory and antioxidant properties and is an active ingredient extracted from the medicinal plant Tanacetum parthenium. ACT001 is derived from parthenolide and is a fumarate form of dimethylaminomylide (DMAMCL). Its effect is equivalent to that of PTL, but it is more stable in plasma and has lower acquisition costs. Related reports indicate that NLRP3-mediated neuroinflammation is involved in the progression of Parkinson's disease (PD). In our research, we explored whether ACT001 alleviates NLRP3-mediated neuroinflammation in PD mice induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). Our results revealed that ACT001 reduces movement impairment and cognitive deficit in PD mice. In addition, it alleviates dopaminergic neurodegeneration in the nigrostriatal pathway and inhibits oxidative stress, the inflammatory response and activation of the NLRP3 inflammasome in the midbrain of MPTP-induced PD mice. Moreover, it attenuates microglial activation in the nigrostriatal pathway. Overall, our study showed that ACT001 alleviates NLRP3-mediated neuroinflammation in PD mice induced by MPTP.