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Preparation, In Vitro and In Vivo Evaluation of Nanoemulsion In Situ Gel for Transnasal Delivery of Traditional Chinese Medicine Volatile Oil from Ligusticum sinense Oliv.cv. Chaxiong.

ABSTRACT: Ischemic stroke is a difficult-to-treat brain disease that may be attributed to a limited therapeutic time window and lack of effective clinical drugs. Nasal-brain administration is characterized by low systemic toxicity and is a direct and non-invasive brain targeting route. Preliminary studies have shown that the volatile oil of Chaxiong (VOC) has an obvious anti-ischemic stroke effect. In this work, we designed a nanoemulsion thermosensitive in situ gel (VOC-NE-ISG) loaded with volatile oil of Chaxiong for ischemia via intranasal delivery to rat brain treatment of cerebral ischemic stroke. The developed VOC-NE-ISG formulation has a suitable particle size of 21.02 ± 0.25 nm and a zeta potential of -20.4 ± 1.47 mV, with good gelling ability and prolonged release of the five components of VOC. The results of in vivo pharmacokinetic studies and brain targeting studies showed that intranasal administration of VOC-NE-ISG could significantly improve the bioavailability and had excellent brain-targeting efficacy of nasal-to-brain delivery. In addition, the results of pharmacodynamics experiments showed that both VOC-NE and VOC-NE-ISG could reduce the neurological deficit score of model rats, reducing the size of cerebral infarction, with a significant effect on improving ischemic stroke. Overall, VOC-NE-ISG may be a promising intranasal nanomedicine for the effective treatment of ischemic stroke.

SUBMITTER: Huang C

PROVIDER: S-EPMC9655233 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature

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Preparation, In Vitro and In Vivo Evaluation of Nanoemulsion In Situ Gel for Transnasal Delivery of Traditional Chinese Medicine Volatile Oil from <i>Ligusticum sinense</i> Oliv.cv. Chaxiong.

Huang Chunhui C Wang Canjian C Zhang Wenliu W Yang Tao T Xia Mingyan M Lei Xiaomeng X Peng Ying Y Wu Yuhuan Y Feng Jianfang J Li Dongxun D Zhang Guosong G

Molecules (Basel, Switzerland) 20221107 21

Ischemic stroke is a difficult-to-treat brain disease that may be attributed to a limited therapeutic time window and lack of effective clinical drugs. Nasal-brain administration is characterized by low systemic toxicity and is a direct and non-invasive brain targeting route. Preliminary studies have shown that the volatile oil of Chaxiong (VOC) has an obvious anti-ischemic stroke effect. In this work, we designed a nanoemulsion thermosensitive in situ gel (VOC-NE-ISG) loaded with volatile oil o ...[more]

PMID: 36364473

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Project description:Ligusticum sinense cv. Chuanxiong (L. Chuanxiong), one of the widely used traditional Chinese medicines (TCM), is currently facing the problem of excessive cadmium (Cd) content. This problem has significantly affected the quality and safety of L. Chuanxiong and become a vital factor restricting its clinical application and international trade development. Currently, to solve the problem of excessive Cd, it is essential to research the response mechanisms of L. Chuanxiong to Cd stress. However, there are few reports on its physiological and biochemical responses under Cd stress. In this study, we conducted the hydroponic experiment under 25 μM Cd stress, based on the Cd content of the genuine producing areas soil. The results showed that 25 μM Cd stress not only had no significant inhibitory effect on the growth of L. Chuanxiong seedlings but also significantly increased the chlorophyll a content (11.79%) and root activity (51.82%) compared with that of the control, which might be a hormesis effect. Further results showed that the absorption and assimilation of NH4+ increased in seedlings under 25 μM Cd stress, which was associated with high photosynthetic pigments. Here, we initially hypothesized and confirmed that Cd exceedance in the root system of L. Chuanxiong was due to the thickening of the root cell wall, changes in the content of the cell wall components, and chelation of Cd by GSH. There was an increase in cell wall thickness (57.64 %) and a significant increase in cellulose (25.48%) content of roots under 25 μM Cd stress. In addition, L. Chuanxiong reduced oxidative stress caused by 25 μM Cd stress mainly through the GSH/GSSG cycle. Among them, GSH-Px (48.26%) and GR (42.64%) activities were significantly increased, thereby maintaining a high GSH/GSSG ratio. This study preliminarily reveals the response of L. Chuanxiong to Cd stress and the mechanism of Cd enrichment. It provides a theoretical basis for solving the problem of Cd excessive in L. Chuanxiong.

Project description:BACKGROUND:There are a lot of different types of sunscreen products (oils, sticks, gels, creams, lotions) which can be found on the world's market. Sunscreen product that contains active chemical ingredients sometimes has harmful effects on the skin. Sunflower oil contains vitamin E and acts as a natural sunscreen which can absorb UVB light. The average droplet size of nanoemulsion is between 100 and 500 nm and do not show the problems of stability (creaming, flocculation, coalescence, and sedimentation), which are commonly associated with macroemulsions. AIM:The aim of this study was to prepare and evaluate the sunflower oil nanoemulsion as a sunscreen. METHODS:Sunflower oil nanoemulsions were prepared by spontaneous emulsification method with 3 formulas F1 (Tween 80 38%, sorbitol 22%), F2 (Tween 80 36%, sorbitol 24%), F3 (Tween 80 34%, sorbitol 26%) and 5% sunflower oil as a sunscreen substance. The nanoemulsions were evaluated for particle size, physical stability in room temperature (25 ± 2°C), low temperature (4 ± 2°C) and high temperature (40 ± 2°C) during experiment for 12 weeks of storage, centrifugation at 3750 rpm for 5 hours, viscosity, pH, freeze-thaw test and sun protection value (SPF) value by in vitro. RESULTS:The results of nanoemulsion evaluation showed that nanoemulsion formula F1 had the smallest average particle size of 124.47 nm with yellowish colour, clear, transparent, pH value (6.5 ± 0.1), viscosity value (225 ± 25 cP), did not show any separation or creaming in the centrifugation, and stable during experiment for 12 weeks of storage at room temperature, low temperature and high temperature. The SPF value of all nanoemulsion preparations was higher than that of the emulsion. CONCLUSION:The preparation of the sunflower oil nanoemulsion with a ratio of Tween 80 and sorbitol (38: 22) produces a stable nanoemulsion during the experiment for 12 weeks storage at the room, low and high temperature. The nanoemulsion preparation has higher SPF values compared to the emulsion. This nanoemulsion formulation could be considered more effective in sunscreen cosmetic use compare to the emulsion.

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Dataset Information

Preparation, In Vitro and In Vivo Evaluation of Nanoemulsion In Situ Gel for Transnasal Delivery of Traditional Chinese Medicine Volatile Oil from Ligusticum sinense Oliv.cv. Chaxiong.

Publications

Preparation, In Vitro and In Vivo Evaluation of Nanoemulsion In Situ Gel for Transnasal Delivery of Traditional Chinese Medicine Volatile Oil from <i>Ligusticum sinense</i> Oliv.cv. Chaxiong.

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