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Intranasal delivery of paeoniflorin nanocrystals for brain targeting

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Asian Journal of Pharmaceutical Sciences 2020年第3期15卷 326-335页

作者： Chaoyin Wu Benyue Li Yi Zhang Tingting Chen Chuangrong Chen Wei Jiang Qi Wang Tongkai Chen Institute of Clinical Pharmacology Guangzhou University of Chinese MedicineGuangzhou 510405China Guangzhou Institutes of Biomedicine and Health Chinese Academy of SciencesGuangzhou 510530China Science and Technology Department Guangzhou University of Chinese MedicineGuangzhou 510006China Department of Radiology Sun Yet-sen Memorial HospitalSun Yet-sen UniversityGuangzhou 510120China

Paeoniflorin(PA) is an anti-Parkinson Chinese medicine with inferior bioavailability and difficulty in delivery to the brain. This research is to develop an efficacious PA nanocrystal formulation(PA-NCs) that is suitable for intranasal administration to treat Parkinson’s disease(PD). PA-NCs were fabricated through an antisolvent precipitation method using TPGS as the stabilizer. The rod-shaped PA-NCs had particle size of 139.6 ± 1.3 nm and zeta potential of-23.2 ± 0.529 mV. A molecular dynamics simulation indicated that van der Waals forces are the primary drivers of interactions between PA and TPGS. In the ex vivo nasal mucosa permeation assay, the cumulative drug release at 24 h was 87.14% ± 5.34%,which was significantly higher than that of free PA. PA-NCs exhibited substantially improved cellular uptake as well as permeability on Calu-3 cells as compared to PA alone. FRET imaging analysis demonstrated that intact NCs could be internalized into Calu-3 cells.Moreover, PA-NCs conferred desirable protective effect against MPP+-induced SH-SY5Y cellular damage. Pharmacokinetic studies revealed a higher PA concentration in the brain following intranasal delivery of PA-NCs. In summary, the intranasal administration of PANCs is a promising treatment strategy for PD.

关键词： Intranasal delivery Nanocrystals Paeoniflorin brain targeting Neuroprotective effect

Development and evaluation of vinpocetine inclusion complex for brain targeting

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Asian Journal of Pharmaceutical Sciences 2015年第2期10卷 114-120页

作者： Jiaojiao Ding Jinfeng Li Shirui Mao School of Pharmacy Shenyang Pharmaceutical UniversityShenyang 110016China

The objective of this paper is to prepare vinpocetine(VIN)inclusion complex and evaluate its brain targeting effect after intranasal administration.In the present study,VIN inclusion complex was prepared in order to increase its solubility.Stability constant(Kc)was used for host selection.Factors influencing properties of the inclusion complex was investigated.Formation of the inclusion complex was identified by solubility study and DSC analysis.The brain targeting effect of the complex after intranasal administration was studied in rats.It was demonstrated that properties of the inclusion complex was mainly influenced by cyclodextrin type,organic acids type,system pH and host/guest molar ratio.Multiple component complexes can be formed by the addition of citric acid,with solubility improved for more than 23 times.Furthermore,In vivo study revealed that after intranasal administration,the absolute bioavailability of vinpocetine inclusion complex was 88%.Compared with intravenous injection,significant brain targeting effect was achieved after intranasal delivery,with brain targeting index 1.67.In conclusion,by intranasal administration of VIN inclusion complex,a fast onset of action and good brain targeting effect can be achieved.Intranasal route is a promising approach for the treatment of CNS diseases.

关键词： Vinpocetine Hydroxypropyl-b-cyclodextrin Citric acid Inclusion complex brain targeting

brain-targeted polymersome codelivery of siRNA and temozolomide for effective glioblastoma chemo-RNAi synergistic therapy

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ChemPhysMater 2022年第3期1卷 203-210页

作者： Meng Zheng Chengnan Yan Qingshan Yang Feiyan Zhu Qiuli Du Xue Xia Marco Morsch Albert Lee Jinglong Yin Yan Zou Bingyang Shi Henan-Macquarie University Joint Centre for Biomedical Innovation School of Life SciencesHenan UniversityKaifeng 475004China Henan Key Laboratory of brain Targeted Bio-nanomedicine School of Life Sciences and School of PharmacyHenan UniversityKaifeng 475004China Department of Biomedical Sciences Faculty of MedicineHealth and Human SciencesMacquarie UniversitySydneyAustralia

Temozolomide (TMZ) is a clinically approved drug for glioblastoma (GBM) therapy. However, as a result of methylguanine-DNA-methyltransferase (MGMT), which is able to repair damaged DNA-damage repairing, TMZ usually yields unsatisfactory therapeutic effects. Small interfering RNA (siRNA) is a potential alteration tool for sensitivity of TMZ by targeting DNA repair enzymes. However, a suitable TMZ and siRNA codelivery system that can effectively and actively co-deliver siRNA/TMZ into the brain tumor is lacking. In this study, we constructed an angiopep-2 decorated polymersomal delivery system to co-deliver TMZ/siRNA for synergistic GBM therapy. This targeted polymersomal nanomedicine not only enhanced the circulation time of siRNA/TMZ in blood but also improved their blood-brain barrier (BBB) crossing and GBM targeting ability. Moreover, when we co-administered siRNAs specific to retinoblastoma binding protein 4 (RBBP4) together with TMZ in GBM cells, these RBBP4- specific siRNA (siRBBP4) modulated the sensitivity of TMZ by regulating MGMT, and thus showed a powerful synergistic anti-tumor effect. We demonstrated that angiopep-2 decorated polymersomal siRBBP4/TMZ co-loaded nanomedicines are capable of inhibiting tumor growth and significantly improved life expectancy of orthotropic GBM bearing mice. Overall, our study suggests that such a polymersomal TMZ/siRNA codelivery system provides a robust and potent nanoplatform for targeted GBM chemo-RNAi therapy.

关键词： Polymersome siRNA TMZ Glioblastoma brain targeting

Lactoferrin modification of berberine nanoliposomes enhances the neuroprotective effects in a mouse model of Alzheimer’s disease

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Neural Regeneration Research 2023年第1期18卷 226-232页

作者： Lin Wang Bi-Qiang Zhou Ying-Hong Li Qian-Qian Jiang Wei-Hong Cong Ke-Ji Chen Xiao-Min Wen Zheng-Zhi Wu The First Affiliated Hospital of Shenzhen University Shenzhen Second People’s HospitalShenzhen Institute of GeriatricsShenzhenGuangdong ProvinceChina The First Affiliated Hospital of Shenzhen University Shenzhen Second People’s HospitalShenzhenGuangdong ProvinceChina China Academy of Chinese Medical Sciences Xiyuan HospitalBeijingChina School of Chinese Medicine Southern Medical UniversityGuangzhouGuangdong ProvinceChina

Previous studies have shown that berberine has neuroprotective effects against Alzheimer’s disease,including antagonizing tau phosphorylation,and inhibiting acetylcholinesterase activity and neural cell apoptosis.However,its low bioavailability and adverse reactions with conventional administration limit its clinical application.In this study,we prepared berberine nanoliposomes using liposomes characterized by low toxicity,high entrapment efficiency,and biodegradability,and modified them with lactoferrin.Lactoferrin-modified berberine nanoliposomes had uniform particle size and high entrapment efficiency.We used the lactoferrin-modified berberine nanoliposomes to treat a mouse model of Alzheimer’s disease established by injection of amyloid-beta 1-42 into the lateral ventricle.Lactoferrin-modified berberine nanoliposomes inhibited acetylcholinesterase activity and apoptosis in the hippocampus,reduced tau over-phosphorylation in the cerebral cortex,and improved mouse behavior.These findings suggest that modification with lactoferrin can enhance the neuroprotective effects of berberine nanoliposomes in Alzheimer’s disease.

关键词： acetylcholinesterase Alzheimer’s disease apoptosis berberine brain targeting lactoferrin nanoliposomes neuroprotective effects Tau phosphorylation

Exploring the potential to enhance drug distribution in the brain subregion via intranasal delivery of nanoemulsion in combination with borneol as a guider

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Asian Journal of Pharmaceutical Sciences 2023年第6期18卷 175-187页

作者： Xin Shen Zhixiang Cui Yidan Wei Yingnan Huo Duo Yu Xin Zhang Shirui Mao School of Pharmacy Shenyang Pharmaceutical UniversityShenyang 110016China

The number of people with Alzheimer’s disease(AD)is increasing annually,with the nidus mainly concentrated in the cortex and hippocampus.Despite of numerous efforts,effective treatment of AD is still facing great challenges due to the blood brain barrier(BBB)and limited drug distribution in the AD nidus sites.Thus,in this study,using vinpocetine(VIN)as a model drug,the objective is to explore the feasibility of tackling the above bottleneck via intranasal drug delivery in combination with a brain guider,borneol(BOR),using nanoemulsion(NE)as the carrier.First of all,the NE were prepared and characterized.In vivo behavior of the NE after intranasal administration was investigated.Influence of BOR dose,BOR administration route on drug brain targeting behavior was evaluated,and the influence of BOR addition on drug brain subregion distribution was probed.It was demonstrated that all the NE had comparable size and similar retention behavior after intranasal delivery.Compared to intravenous injection,improved brain targeting effect was observed by intranasal route,and drug targeting index(DTI)of the VIN–NE group was 154.1%,with the nose-to-brain direct transport percentage(DTP)35.1%.Especially,remarkably enhanced brain distribution was achieved after BOR addition in the NE,with the extent depending on BOR dose.VIN brain concentration was the highest in the VIN-1-BOR-NE group at BOR dose of 1 mg/kg,with the DTI reaching 596.1%and the DTP increased to 83.1%.BOR could exert better nose to brain delivery when administrated together with the drug via intranasal route.Notably,BOR can remarkably enhance drug distribution in both hippocampus and cortex,the nidus areas of AD.In conclusion,in combination with intranasal delivery and the intrinsic brain guiding effect of BOR,drug distribution not only in the brain but also in the cortex and hippocampus can be enhanced significantly,providing the perquisite for improved therapeutic efficacy of AD.

关键词： Vinpocetine Borneol Nanoemulsions Intranasal administration brain targeting brain subregion distribution

Solid lipid nanoparticles for nose to brain delivery of haloperidol:in vitro drug release and pharmacokinetics evaluation

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Acta Pharmaceutica Sinica B 2014年第6期4卷 454-463页

作者： Mohd Yasir Udai Vir Singh Sara Department of Pharmacy Uttarakhand Technical UniversityDehradun 248007UttarakhandIndia Department of Pharmaceutics ITS Pharmacy CollegeMuradnagarGhaziabad 201206Uttar PradeshIndia College of Pharmaceutical Sciences Raj Kumar Goel Institute of TechnologyGhaziabad 201201Uttar PradeshIndia

In the present study,haloperidol(HP)-loaded solid lipid nanoparticles(SLNs)were prepared to enhance the uptake of HP to brain via intranasal(i.n.)delivery.SLNs were prepared by a modified emulsification-diffusion technique and evaluated for particle size,zeta potential,drug entrapment efficiency,in vitro drug release,and stability.All parameters were found to be in an acceptable range.In vitro drug release was found to be 94.1674.78%after 24 h and was fitted to the Higuchi model with a very high correlation coefficient(R2¼0.9941).Pharmacokinetics studies were performed on albino Wistar rats and the concentration of HP in brain and blood was measured by high performance liquid chromatography.The brain/blood ratio at 0.5 h for HP-SLNs i.n.,HP sol.***.n.and HP sol.***.v.was 1.61,0.17 and 0.031,respectively,indicating direct nose-to-brain transport,bypassing the blood-brain barrier.The maximum concentration(Cmax)in brain achieved from i.***.administration of HP-SLNs(329.17720.89 ng/mL,Tmax 2 h)was significantly higher than that achieved after i.v.(76.9577.62 ng/mL,Tmax 1 h),and i.n.(90.1376.28 ng/mL,Tmax 2 h)administration of HP sol.The highest drug-targeting efficiency(2362.43%)and direct transport percentage(95.77%)was found with HP-SLNs as compared to the other formulations.Higher DTE(%)and DTP(%)suggest that HP-SLNs have better brain targeting efficiency as compared to other formulations.

关键词： brain targeting Haloperidol Intranasal route Pharmacokinetics Solid lipid nanoparticles

Effect of borneol and electroacupuncture on the distribution of hyperforin in the rat brain

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Neural Regeneration Research 2011年第24期6卷 1876-1882页

作者： Bin Yu Ming Ruan Yong Sun Xiaobing Cui Yun Yu Lingling Wang Taihui Fang Key Laboratory of Integrative Acupuncture and Drugs Constructed by Jiangsu Provincial and Chinese Education Ministry Nanjing University of Traditional Chinese Medicine Nanjing 210046 Jiangsu Province China Department of Pharmacy Nanjing University of Traditional Chinese Medicine Nanjing 210046 Jiangsu Province China Department of Life Science Nanjing Xiaozhuang College Nanjing 211171 Jiangsu Province China

Hyperforin is an antidepressant drug that has unstable therapeutic effects, due to its poor ability to cross the blood-brain barrier. Borneol and electroacupuncture have both been found to increase the permeability of the blood-brain barrier. As such, the current study examined the distribution of hyperforin in the rat brain, and the effects on the brain distribution of hyperforin of borneol alone （orally administered）, and borneol combined with electroacupuncture treatment. High-performance liquid chromatography technology and pharmacokinetic analysis revealed that treatment with borneol alone （300, 600 mg/kg） increased peak concentration and the area under the curve for hyperforin in the brain. In addition, the bioavailability of hyperforin in rat brain increased by 42.7%. However, increasing the dose of borneol dose did not appear to increase the distribution of hyperforin in the brain. Importantly, applying electroacupuncture at Baihui （GV 20） or Yamen （GV 15） appeared to enhance the brain-delivery effects of borneol, although this effect was weak. Overall, our results indicated that borneol alone or combined with electroacupuncture can provide promising strategies for brain-targeted delivery in central nervous system therapy.

关键词： hyperforin borneol electroacupuncture blood-brain barrier brain targeting neural regeneration

brain-targeted drug delivery assisted by physical techniques and its potential applications in traditional Chinese medicine

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Journal of Traditional Chinese Medical Sciences 2021年第3期8卷 186-197页

作者： Yunbo Sun Lina Du Meiyan Yang Qi Li Xueli Jia Qian Li Lin Zhu Yuanyuan Zhang Yijing Liu Shuchen Liu Department of Pharmaceutics Beijing Institute of Radiation MedicineBeijing100850China School of Pharmacy Shandong University of Traditional Chinese MedicineJinan250300China State Key Laboratory of Toxicology and Medical Countermeasures Beijing Institute of Pharmacology and ToxicologyJinan250300China

The blood-brain barrier(BBB)constitutes a major obstacle to effective delivery of drugs to the brain.Recent technological advances have led to improvements in brain-targeted drug delivery.In this review,we summarize existing technologies for efficient drug delivery across the BBB.We discuss the mechanisms of current BBB-based drug delivery strategies and introduce prospects for application in braint-argeted delivery of traditional Chinese medicine.We highlight the use of physical techniques for brain-targeted drug delivery,including electroporation,ultrasound,magnetophoresis,microneedles,microwaves,and laser.The characteristics of these techniques and relevant studies employing these approaches are discussed.In general,microneedles,lasers,ultrasound,electroporation,magnetophoresis,and microwaves are effective for drug delivery across the BBB.Notably,the synergistic effects of multiple approaches are superior to the additive effects of each technique in isolation.Our review provides guidance for the practical application of brain-targeted drug delivery techniques in an efficient and safe manner.

关键词： Blood-brain barrier Physical techniques Drug delivery brain targeting

Intranasal temperature-sensitive hydrogels of cannabidiol inclusion complex for the treatment of post-traumatic stress disorder

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Acta Pharmaceutica Sinica B 2021年第7期11卷 2031-2047页

作者： Lulu Pang Siqing Zhu Jinqiu Ma Lin Zhu Yijing Liu Ge Ou Ruiteng Li Yaxin Wang Yi Liang Xu Jin Lina Du Yiguang Jin Department of Pharmaceutical Sciences Beijing Institute of Radiation MedicineBeijing 100850China College of Pharmacy Shandong University of Traditional Chinese MedicineJinan 250355China College of Pharmacy Anhui Medical UniversityHefei 230001China Pharmacy Department Chinese PLA General HospitalBeijing 100853China Department of Anesthesiology Beijing Tiantan HospitalCapital Medical UniversityBeijing 100070China

Post-traumatic stress disorder(PTSD)is a psychiatric disease that seriously affects brain function.Currently,selective serotonin reuptake inhibitors(SSRIs)are used to treat PTSD clinically but have decreased efficiency and increased side effects.In this study,nasal cannabidiol inclusion complex temperature-sensitive hydrogels(CBD TSGs)were prepared and evaluated to treat PTSD.Mice model of PTSD was established with conditional fear box.CBD TSGs could significantly improve the spontaneous behavior,exploratory spirit and alleviate tension in open field box,relieve anxiety and tension in elevated plus maze,and reduce the freezing time.Hematoxylin and eosin and c-FOS immunohistochemistry slides showed that the main injured brain areas in PTSD were the prefrontal cortex,amygdala,and hippocampus CA1.CBD TSGs could reduce the level of tumor necrosis factor-a caused by PTSD.Western blot analysis showed that CBD TSGs increased the expression of the 5-HT1 A receptor.Intranasal administration of CBD TSGs was more efficient and had more obvious brain targeting effects than oral administration,as evidenced by the pharmacokinetics and brain tissue distribution of CBD TSGs.Overall,nasal CBD TSGs are safe and effective and have controlled release.There are a novel promising option for the clinical treatment of PTSD.

关键词： Post-traumatic stress disorder Cannabidiol Hydroxypropyl-β-cyclodextrin Inclusion complex Hydrogels brain targeting Blood-brain barrier Intranasal administration