Neurodegenerative diseases(NDs)are a major threat to the elderly,and efficient therapy is rarely available.A group of phytochemicals has been shown to ameliorate NDs;however,poor stability,low bioavailability,and redu...Neurodegenerative diseases(NDs)are a major threat to the elderly,and efficient therapy is rarely available.A group of phytochemicals has been shown to ameliorate NDs;however,poor stability,low bioavailability,and reduced drug accumulation in brain tissue limit their application in NDs.Therefore,a targeted drug delivery system is a feasible treatment strategy for NDs.Extracellular vesicles(EVs)possess many favorable bioactivities and are excellent carriers for targeting brain tissue.This review summarizes EVs as novel phytochemical carriers in ND therapy.First,we discuss the current challenges of ND therapy and the therapeutic effects of phytochemicals for NDs.Second,we highlight the ability of EVs to cross the blood-brain barrier and act as drug carriers to enhance the therapeutic efficacy of drugs for NDs.Finally,encapsulation strategies for phytochemicals in EVs are particularly reviewed,as they are critical for obtaining high loading efficacy and stable drug delivery systems.This review provides new insights into EV-based drug delivery systems for improving the therapeutic effect of phytochemicals for ND treatment.Therefore,the release rate and pharmacokinetics of phytochemicals should be well controlled to ensure the therapeutic efficacy of phytochemical-loaded EVs in the brain.展开更多
In the present study,we aimed to probe the possibility of using mixed poloxamers as carriers to prepare ternary solid dispersion(SD)that facilitated solubility and dissolution rate of the poorly water soluble drug and...In the present study,we aimed to probe the possibility of using mixed poloxamers as carriers to prepare ternary solid dispersion(SD)that facilitated solubility and dissolution rate of the poorly water soluble drug and compare with binary SD with single poloxamer.Lidocaine(LIC)was selected as a model drug,and poloxamer 188(P188)and poloxamer 407(P407)were utilized as single and mixed carriers.Depending on DSC and the dissolution testing,the appropriate ratio of SD prepared by melting method was optimized.Ternary and binary SD was characterized by DSC,XRD,SEM and FTIR.In vitro dissolution study,phase solubility study and saturated solubility study were performed to clarify solubilization from apparent phenomena and inherent reason.Moreover,stability study under different relative humidity(RH)was investigated.Physical characterizations of binary and ternary SD exhibited the formation of eutectic mixture and the presence of molecular interaction.Compared with the pure LIC,the dissolution rate and solubility of LIC in binary and ternary SDs were enhanced.The phase solubility study revealed an AL-type curve.Furthermore,the stability test indicated that ternary and binary SD was stable.The results of this study demonstrated that SD with mixed poloxamers could improve dissolution rate and solubility of poorly water-soluble drug.展开更多
基金supported by the National Natural Science Foundation of China(Grant 31700714)the Young Scholars Supporting Program of Nanjing University of Finance and Economics(Grant ZZZXW20001)the Priority Academic Program Development of Jiangsu Higher Education Institutions
文摘Neurodegenerative diseases(NDs)are a major threat to the elderly,and efficient therapy is rarely available.A group of phytochemicals has been shown to ameliorate NDs;however,poor stability,low bioavailability,and reduced drug accumulation in brain tissue limit their application in NDs.Therefore,a targeted drug delivery system is a feasible treatment strategy for NDs.Extracellular vesicles(EVs)possess many favorable bioactivities and are excellent carriers for targeting brain tissue.This review summarizes EVs as novel phytochemical carriers in ND therapy.First,we discuss the current challenges of ND therapy and the therapeutic effects of phytochemicals for NDs.Second,we highlight the ability of EVs to cross the blood-brain barrier and act as drug carriers to enhance the therapeutic efficacy of drugs for NDs.Finally,encapsulation strategies for phytochemicals in EVs are particularly reviewed,as they are critical for obtaining high loading efficacy and stable drug delivery systems.This review provides new insights into EV-based drug delivery systems for improving the therapeutic effect of phytochemicals for ND treatment.Therefore,the release rate and pharmacokinetics of phytochemicals should be well controlled to ensure the therapeutic efficacy of phytochemical-loaded EVs in the brain.
基金National Natural Science Fund of China(Grant No.30801552&81274095)the third key project funded by Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization(Grant No.012092002006-10)the 55th postdoctoral project(Grant No.021062001001).
文摘In the present study,we aimed to probe the possibility of using mixed poloxamers as carriers to prepare ternary solid dispersion(SD)that facilitated solubility and dissolution rate of the poorly water soluble drug and compare with binary SD with single poloxamer.Lidocaine(LIC)was selected as a model drug,and poloxamer 188(P188)and poloxamer 407(P407)were utilized as single and mixed carriers.Depending on DSC and the dissolution testing,the appropriate ratio of SD prepared by melting method was optimized.Ternary and binary SD was characterized by DSC,XRD,SEM and FTIR.In vitro dissolution study,phase solubility study and saturated solubility study were performed to clarify solubilization from apparent phenomena and inherent reason.Moreover,stability study under different relative humidity(RH)was investigated.Physical characterizations of binary and ternary SD exhibited the formation of eutectic mixture and the presence of molecular interaction.Compared with the pure LIC,the dissolution rate and solubility of LIC in binary and ternary SDs were enhanced.The phase solubility study revealed an AL-type curve.Furthermore,the stability test indicated that ternary and binary SD was stable.The results of this study demonstrated that SD with mixed poloxamers could improve dissolution rate and solubility of poorly water-soluble drug.
