ABSTRACT
ObjectiveTo prepare oral nanoemulsions encapsulating essential oil from Alpinia zerumbet fructus（EOFAZ） and to investigate its pro-absorption effect in vitro and distribution in vivo. MethodThe proteoglycan conjugate polysaccharides of vinegar-processed Bupleuri Radix-bovine serum albumin（VBCP-BSA） was prepared by Maillard reaction of VBCP and BSA. Taking VBCP-BSA as emulsifier， vitamin B12（VB12） as absorption enhancer， and medium chain triglycerides mixed with EOFAZ as oil phase， the nanoemulsions loaded with EOFAZ was prepared by high energy emulsification method. The particle size， particle size distribution， surface Zeta potential， EOFAZ content and appearance and morphology of the nanoemulsions were characterized， and fluorescein tracer method was used to investigate the absorption effect of fluorescein-labeled EOFAZ nanoemulsions in vitro and their distribution in vivo. ResultVBCP-BSA was formed by Maillard reaction for 48 h with high grafting rate. Using VBCP-BSA as emulsifier， the homogeneous pink nanoemulsions was prepared and denoted as EOFAZ@VBCP-BSA/VB12. The particle size of the nanoemulsions was less than 100 nm and the particle size distribution was uniform. The surface of the nanoemulsions was a weak negative charge， and the shape was spherical. The encapsulation rate of the nanoemulsions for EOFAZ was greater than 80%， which had a good absorption effect in vitro and could enhance liver accumulation after oral administration. ConclusionThe designed proteoglycan nanoemulsions can effectively load EOFAZ， promote oral absorption and enhance liver distribution， which can provide experimental basis for the development of oral EOFAZ liver protection preparations.
ABSTRACT
To reduce the problems of poor solubility, high in vivo dosage requirement, and weak targeting ability of paclitaxel (PTX), a hyaluronic acid-octadecylamine (HA-ODA)-modified nano-structured lipid carrier (HA-NLC) was constructed. HA-ODA conjugates were synthesized by an amide reaction between HA and ODA. The hydrophobic chain of HA-ODA can be embedded in the lipid core of the NLC to obtain HA-NLC. The HA-NLC displayed strong internalization in cluster determinant 44 (CD44) highly expressed MCF-7 cells, and endocytosis mediated by the CD44 receptor was involved. The HA-NLC had an encapsulation efficiency of PTX of 72.0%. The cytotoxicity of the PTX-loaded nanoparticle HA-NLC/PTX in MCF-7 cells was much stronger than that of the commercial preparation Taxol®. In vivo, the HA-NLC exhibited strong tumor targeting ability. The distribution of the NLCs to the liver and spleen was reduced after HA modification, while more nanoparticles were aggregated to the tumor site. Our results suggest that HA-NLC has excellent properties as a nano drug carrier and potential for in vivo targeting.
ABSTRACT
To reduce the problems of poor solubility, high in vivo dosage requirement, and weak targeting ability of paclitaxel (PTX), a hyaluronic acid-octadecylamine (HA-ODA)-modified nano-structured lipid carrier (HA-NLC) was constructed. HA-ODA conjugates were synthesized by an amide reaction between HA and ODA. The hydrophobic chain of HA-ODA can be embedded in the lipid core of the NLC to obtain HA-NLC. The HA-NLC displayed strong internalization in cluster determinant 44 (CD44) highly expressed MCF-7 cells, and endocytosis mediated by the CD44 receptor was involved. The HA-NLC had an encapsulation efficiency of PTX of 72.0%. The cytotoxicity of the PTX-loaded nanoparticle HA-NLC/PTX in MCF-7 cells was much stronger than that of the commercial preparation Taxol®. In vivo, the HA-NLC exhibited strong tumor targeting ability. The distribution of the NLCs to the liver and spleen was reduced after HA modification, while more nanoparticles were aggregated to the tumor site. Our results suggest that HA-NLC has excellent properties as a nano drug carrier and potential for in vivo targeting.
ABSTRACT
OBJECTIVE: To illustrate and evaluate the properties of folate-targeted liposomes loaded with quantum dots (folate- QDs-liposomes) nanoprobes in vitro and in vivo, such as cytotoxicity, the targeting of folate-QDs-liposomes nanoprobes for tumor cells mediated by the folate-folate receptor pathway, their toxicity in vivo and so on. METHODS: Firstly, the inhibitory effects of folate- QDs-liposomes on cell growth and apoptosis were investigated by MTT and flow cytometry. Secondly, the targeting of folate-QDs-liposomes for folate receptor-positive tumor cells was verified by fluorescence staining. Finally, the epidermal infiltration method was adopted to examine the toxicity and distribution in vivo. RESULTS: Under the same concentration, folate-QDs-liposomes and QDs-liposomes had similar cytotoxicity, and QDs had the most obvious cytotoxicity, which verified that the cytotoxicity of QDs was significantly reduced after liposome coating. In the fluorescence experiment, it was observed that folate-QDs-liposomes targeted at Hela cells, but did not target at A549 cells. Free folic acid could block the specific binding of folate-QDs-liposomes to folate receptors on tumor cells. It was proved that folate-QDs-liposomes could enter tumor cells positively expressing folate receptors through the path of folic acid and folate receptors. In vivo, folate-QDs-liposomes nanoprobes could spread throughout the zebrafish body through the blood circulation system. They were distributed from head and excreted from the tails. CONCLUSION: Folate-QDs-liposomes have potential biomedical application prospects, and can be expected to play an important role in the early detection and diagnosis of tumors.
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Aim To study the distributive character of mitomycin(MMC) magnetic nanoparticles and MMC normal saline solution in mice.Methods A HPLC method for the determination of MMC in tissues and serum were established and applied to determine MMC in biological samples.Results Under the guidance of an external magnetic field,targeting rates of MMC to liver viscus are 82.72% after 30 minutes tail vein administration of(1 mg?kg~(-1)) mitomycin magnetic nanoparticles,it was 2.37 times larger than targeting rates of MMC normal saline solution group.The distributions of heart and kidney of mitomycin magnetic nanoparticles were less than that of MMC normal saline solution group.Compared with the results of tail vein administration mitomycin nanoparticles,interaction between the external magnetic field and magnetic nanoparticles is significantly effective to increase targeting rates of MMC to liver.Compared with the results of tail vein administration mitomycin magnetic nanoparticles without the external magnetic field,Mitomycin magnetic nanoparticles under the guidance of an external magnetic field is significantly effective to increase targeting rates of MMC to liver.Conclusions Mitomycin magnetic nanoparticles under the guidance of an external magnetic field is significantly effective to increase targeting rates of MMC to liver and prolonging effect on the action in vivo.