JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2019
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IF 2.606
Lan Wang,Cai-Yun Wang,Ying Zhang,Hai-Juan Fu,Yan Gao,Ke-Rui Zhang
Salmon calcitonin phospholipid complex loaded-solid lipid nanoparticles (sCT-PC-SLNs) were prepared from Salmon calcitonin phospholipid complex (sCT-PC) by a film dispersion method. The formulation was optimized by the Box-Behnken response surface design using quality properties such as particle size, polydispersity index (PDI), zeta potential value, entrapment efficiency (EE), and drug loading capacity (DL). The relative bioavailability of different dosage forms of salmon calcitonin (sCT) were calculated separately for plasma calcium percentage of SD female rats after subcutaneous injection and colonic administration. The results show that each dosage form offers reduced plasma calcium levels after colonic administration, except for blank loaded-solid lipid nanoparticles (SLN). The relative bioavailability (0.32 ± 0.17%) for sCT-PC-SLN is twice as high as that of aqueous sCT solution (0.16 ± 0.03%), as well as values for Salmon calcitonin loaded-solid lipid nanoparticles (sCT-SLN) (0.15 ± 0.01%); these results are statistically significant. Compared to SLN, uptake of sCT in a rat colon can be greatly improved by phospholipid complex loaded-solid lipid nanoparticles (PC-SLN). The new dosage form developed here overcomes the low EE of the water-soluble drug, enhances the EE of SLN, and reduces the degradation of gastrointestinal enzymes due to its encapsulation in lipids.
研究领域:
药剂学
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生物医学工程
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产品关联
DOI
高影响因子
DRUG DELIVERY
·
2020
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IF 4.902
Yuqi Yang,Yiyue Guo,You Xu,Yingying Meng,Xing Zhang,Xuejun Xia,YuLing Liu
Deformable nanovesicles (DNVs) have been used in the buccal delivery of biomacromolecules due to their ability to enhance drug penetration. However, no breakthroughs have been made until now due to limited understanding of the factors affecting in vivo buccal delivery. In this study, we designed a series of DNVs, based on an insulin–phospholipid complex (IPC-DNVs), to investigate the influence of drug dose, buccal administration methods, and key quality characteristics of IPC-DNVs for buccal delivery. IPC-DNVs showed a non-linear dose–response relationship between 8 and 12 IU. There was no significant effect of drug delivery site (sublingual mucosa/buccal mucosa) or ligation time (15 or 30 min) on buccal absorption of IPC-DNVs. However, the area above the curve of reduction in blood glucose level overtime (AAC0–6h) for oral mucosa administration was significantly higher than that for buccal mucosa administration. Increasing the drug concentration in IPC-DNVs led to a decrease in AAC0–6h. This might be due to local leakage of DNVs, while squeezing through biological barriers with high concentration of insulin, thus hindering the subsequent delivery of DNVs. IPC-DNVs, measuring 80–220 nm in size, did not significantly affect AAC0–6h. However, when the size was increased to approximately 400 nm, AAC0–6h decreased, thus suggesting that IPC-DNVs with reasonable size were more effective. Additionally, increased deformability of IPC-DNVs might cause drugs to leak easily, thus reducing the promoting effect of buccal absorption. Our results clarified the effect of characteristics of IPC-DNVs on buccal delivery in vivo and provided meaningful support for the design of dosage form of DNVs.
研究领域:
药剂学
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生物医学工程
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药物传递系统
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DOI
PubMed
高影响因子
Bioengineering-Basel
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2024
·Vol. 11
·期 2
·177
·
IF 3.8
Jianhong Liu,Xuyang Lai,Yuanhong Li,Zhuohang Yu,Xuan Wang,Chaoliang Zhang,Qiang Peng
Drug resistance substantially compromises antibiotic therapy and poses a serious threat to public health. Fusidic acid (FA) is commonly used to treat staphylococcal infections, such as pneumonia, osteomyelitis and skin infections. However, Gram-negative bacteria have natural resistance to FA, which is almost restrained in cell membranes due to the strong interactions between FA and phospholipids. Herein, we aim to utilize the strong FA–phospholipid interaction to pre-form a complex of FA with the exogenous phospholipid. The FA, in the form of an FA–phospholipid complex (FA-PC), no longer interacts with the endogenous membrane phospholipids and thus can be delivered into bacteria cells successfully. We found that the water solubility of FA (5 µg/mL) was improved to 133 µg/mL by forming the FA-PC (molar ratio 1:1). Furthermore, upon incubation for 6 h, the FA-PC (20 µg/mL) caused a 99.9% viability loss ofE. coliand 99.1% loss ofP. aeruginosa, while free FA did not work. The morphology of the elongated bacteria cells after treatment with the FA-PC was demonstrated by SEM. The successful intracellular delivery was shown by confocal laser scanning microscopy in the form of coumarin 6-PC (C6-PC), where C6 served as a fluorescent probe. Interestingly, the antibacterial effect of the FA-PC was significantly compromised by adding extra phospholipid in the medium, indicating that there may be a phospholipid-based transmembrane transport mechanism underlying the intracellular delivery of the FA-PC. This is the first report regarding FA-PC formation and its successful reversing of Gram-negative bacteria resistance to FA, and it provides a platform to reverse transmembrane delivery-related drug resistance. The ready availability of phospholipid and the simple preparation allow it to have great potential for clinical use.Keywords:drug delivery;drug resistant;phospholipid complex;antimicrobial;antibiotics
研究领域:
药学
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微生物学
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药物递送系统
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抗菌研究
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DOI
PubMed
高影响因子
POULTRY SCIENCE
·
2019
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IF 2.027
Y. Chen,Y. Yang,F. Wang,X. Yang,F. Yao,K. Ming,W. Yuan,L. Zeng,J. Liu
ABSTRACT Duck hepatitis A virus type 1 ( DHAV-1 ) is one of the main pathogens of ducklings and causes a high mortality rate. Baicalin ( BA ) has potent antiviral effect, but the solubility is very poor. In order to increase the absorption, solubility, and pharmacological activity, the phospholipid complex was used to modify BA in present study. Therefore, BA phospholipid complex ( BAPC ) was prepared. The anti-DHAV-1 abilities of BA and BAPC in vitro was evaluated by cell counting kit-8 and reverse transcription quantitative PCR. The curative effects of BA and BAPC on ducklings which were infected by DHAV-1 in addition to the ALT and AST levels were also detected. The results indicated the anti-DHAV-1 ability of BAPC was stronger than that of BA both in vitro and in vivo . To explore the anti-DHAV-1 mechanism, the influence of BAPC on DHAV-1 adsorption, replication, and release was studied. Furthermore, the anti-oxidative and immuno-enhancing abilities of BAPC in the treatment of infected ducklings were also determined. The results showed BAPC inhibited DHAV-1 adsorption, replication and release. Furthermore, it played anti-oxidative and immno-enhancing roles in the treatment, and the immno-enhancing role was crucial to the treatment.
研究领域:
兽医学
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病毒学
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药理学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）