scholarly journals Drug Nanoparticle Formulation Using Ascorbic Acid Derivatives

2011 ◽  
Vol 2011 ◽  
pp. 1-9 ◽  
Author(s):  
Kunikazu Moribe ◽  
Waree Limwikrant ◽  
Kenjirou Higashi ◽  
Keiji Yamamoto

Drug nanoparticle formulation using ascorbic acid derivatives and its therapeutic uses have recently been introduced. Hydrophilic ascorbic acid derivatives such as ascorbyl glycoside have been used not only as antioxidants but also as food and pharmaceutical excipients. In addition to drug solubilization, drug nanoparticle formation was observed using ascorbyl glycoside. Hydrophobic ascorbic acid derivatives such as ascorbyl mono- and di-n-alkyl fatty acid derivatives are used either as drugs or carrier components. Ascorbyl n-alkyl fatty acid derivatives have been formulated as antioxidants or anticancer drugs for nanoparticle formulations such as micelles, microemulsions, and liposomes. ASC-P vesicles called aspasomes are submicron-sized particles that can encapsulate hydrophilic drugs. Several transdermal and injectable formulations of ascorbyl n-alkyl fatty acid derivatives were used, including ascorbyl palmitate.

2020 ◽  
Vol 17 (4) ◽  
pp. 292-302
Author(s):  
Vicit Rizal Eh Suk ◽  
Ivy Chung ◽  
Misni Misran

Background: Liposomes are mostly known to be prepared from phospholipids and lipids and have a remarkable capacity to encapsulate both lipophobic and lipophilic molecules. However, there is little research on developing fatty acid liposomes for chemotherapy. Objective: We have successfully prepared mixed fatty acid liposomes from two monounsaturated fatty acids, namely oleic acid and erucic acid, which stabilised by DOPEPEG2000. The Critical Vesicular Concentration (CVC) of liposomes was found to be within 0.09 to 0.21 mmol dm-3, with an average particle size of 400 nm. Methods: Encapsulation of various anticancer drugs such as folinic acid, methotrexate, doxorubicin, or irinotecan resulted in Encapsulation Efficiency (%EE) of up to 90%. Using a 3-(4, 5-dimethylthiazol-2- yl)-2,5-diphenyltetrazolium bromide (MTT) assay, the median Inhibitory Concentration (IC50) values of mixed oleic acid-erucic acid encapsulating hydrophilic drugs was remarkably reduced at the end of 24 hours of incubation with the human lung carcinoma cell line A549. Results: The results suggest that mixed oleic acid-erucic acid liposomes are a potential new approach to further develop as an alternative vehicle of various drugs for cancer treatment.


2021 ◽  
Vol 124 ◽  
pp. 195-202
Author(s):  
Jeong-Hun Kim ◽  
Yu-Ri Oh ◽  
Juyoung Hwang ◽  
Jaeryeon Kang ◽  
Hyeri Kim ◽  
...  

2021 ◽  
Vol 86 (5) ◽  
pp. 3970-3980
Author(s):  
Kenji Sugimoto ◽  
Ami Kobayashi ◽  
Aki Kohyama ◽  
Haruka Sakai ◽  
Yuji Matsuya

2021 ◽  
Vol 22 (6) ◽  
pp. 3106
Author(s):  
Giada Bianchetti ◽  
Salome Azoulay-Ginsburg ◽  
Nimrod Yosef Keshet-Levy ◽  
Aviv Malka ◽  
Sofia Zilber ◽  
...  

Free fatty acids are essential structural components of the cell, and their intracellular distribution and effects on membrane organelles have crucial roles in regulating the metabolism, development, and cell cycle of most cell types. Here we engineered novel fluorescent, polarity-sensitive fatty acid derivatives, with the fatty acid aliphatic chain of increasing length (from 12 to 18 carbons). As in the laurdan probe, the lipophilic acyl tail is connected to the environmentally sensitive dimethylaminonaphthalene moiety. The fluorescence lifetime imaging analysis allowed us to monitor the intracellular distribution of the free fatty acids within the cell, and to simultaneously examine how the fluidity and the microviscosity of the membrane environment influence their localization. Each of these probes can thus be used to investigate the membrane fluidity regulation of the correspondent fatty acid intracellular distribution. We observed that, in PC-12 cells, fluorescent sensitive fatty acid derivatives with increased chain length compartmentalize more preferentially in the fluid regions, characterized by a low microviscosity. Moreover, fatty acid derivatives with the longest chain compartmentalize in lipid droplets and lysosomes with characteristic lifetimes, thus making these probes a promising tool for monitoring lipophagy and related events.


2014 ◽  
Vol 24 (2) ◽  
pp. 604-608 ◽  
Author(s):  
Hong-Yan Zhang ◽  
Yu-ichiro Yamakawa ◽  
Yuji Matsuya ◽  
Naoki Toyooka ◽  
Chihiro Tohda ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document