Polymeric micelles deliver phthalocyanine for enhancement in vitro photodynamic efficacy

Author(s):  
Ruotao Guo ◽  
Shuanghuang Xiao ◽  
Qiaohao Ye ◽  
Yiru Peng ◽  
Kuizhi Chen ◽  
...  
Keyword(s):  
Author(s):  
R S Thakur ◽  
A Nayaz ◽  
Y Koushik

In the case of solubility limited absorption, creating supersaturation in the GI fluid is very critical as supersaturation may provide great improvement of oral absorption. The techniques to create the so-called supersaturation in the GI fluid include microemulsions, emulsions, liposomes, complexations, polymeric micelles, and conventional micelles. Ciprofloxacin was chosen because it is practically insoluble in water; hence its salt form is used commercially, which is soluble in water. The objective of the present investigation was to enhance the solubility of Ciprofloxacin by formulating it into microemulsion system. For this purpose, initially, surfactant and cosurfactant were selected based on their HLB value, followed by pseudo-ternary phase diagrams to identify the microemulsion existing zone. Different formulations were developed and evaluated for pH, conductivity, in vitro release and stability. Solubility study was performed for optimized formulation. The pH of the designed formulations varied from 6.02-7.04. This was ideal and near blood pH 7.4. Conductivity data indicated that the microemulsion was of the o/w type. In vitro release of optimized formulation(FM3) was 95.2% as compared to pure drug 46.61% after 90 min and marketed product(salt form) 93.9%. Hence, by formulating into microemulsion, the solubility of ciprofloxacin is significantly enhanced.    


Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 186
Author(s):  
Maria Natalia Calienni ◽  
Daniela Maza Vega ◽  
C. Facundo Temprana ◽  
María Cecilia Izquierdo ◽  
David E. Ybarra ◽  
...  

Vismodegib is a first-in-class inhibitor for advanced basal cell carcinoma treatment. Its daily oral doses present a high distribution volume and several side effects. We evaluated its skin penetration loaded in diverse nanosystems as potential strategies to reduce side effects and drug quantities. Ultradeformable liposomes, ethosomes, colloidal liquid crystals, and dendrimers were able to transport Vismodegib to deep skin layers, while polymeric micelles failed at this. As lipidic systems were the most effective, we assessed the in vitro and in vivo toxicity of Vismodegib-loaded ultradeformable liposomes, apoptosis, and cellular uptake. Vismodegib emerges as a versatile drug that can be loaded in several delivery systems for topical application. These findings may be also useful for the consideration of topical delivery of other drugs with a low water solubility.


2000 ◽  
Vol 205 (1-2) ◽  
pp. 165-172 ◽  
Author(s):  
In-Sook Kim ◽  
Young-Il Jeong ◽  
Chong-Su Cho ◽  
Sung-Ho Kim

2020 ◽  
Vol 21 (8) ◽  
Author(s):  
Mohamed Nasr ◽  
Fahima Hashem ◽  
Raghda Abdelmoniem ◽  
Norhan Tantawy ◽  
Mohamed Teiama

2014 ◽  
Vol 430 ◽  
pp. 305-314 ◽  
Author(s):  
Partha Laskar ◽  
Sintu Samanta ◽  
Sudip Kumar Ghosh ◽  
Joykrishna Dey

2019 ◽  
Vol 15 (7) ◽  
pp. 1515-1531 ◽  
Author(s):  
Zejiang Zhu ◽  
Zhengying Su ◽  
Jianhong Yang ◽  
Huili Liu ◽  
Minghai Tang ◽  
...  

In our previous study, we identified a class of 4-substituted coumarins as a powerful microtubule inhibitors binding to the colchicine site of β-tubulin. H6 showed potent anti-proliferative ability with IC50 values from 7 to 47 nM, and remarkable ability to reduce tumor growth in several xenograft models including taxol resistant tumor models. However, the extremely hydrophobicity limited its clinical application. In this study, to improve the anticancer activity and reduce the toxicity of H6, we successfully prepared MPEG-PCL with different proportions and H6-loaded polymeric micelles (H6/MPEG2kPCL2k micelles) by a simple thin-film hydration method. The prepared H6/MPEG-PCL micelles had a drug loading of 3.79 ± 0.001%, an encapsulation efficiency of 98.00 ± 0.41%, a mean particle size of 30.45 ± 0.18nm and a polydispersity index (PDI) of 0.096 ± 0.009. Computer simulation results revealed a good compatibility of H6 and MPEG2k-PCL2k copolymer. In in vitro release study and pharmacokinetic study showed H6 micelles can release H6 over an extended period. Furthermore, H6 micelles possessed comparative effect as free H6 in inhibiting cell growth, preventing cell migration, and inducing apoptosis. Mechanism study identified that H6 is a novel reversible microtubule inhibitor. In in vivo studies, H6 micelles exhibited tumor growth inhibition on two pulmonary metastatic tumor models (B16/F10 and 4T1). Importantly, H6 micelles significantly improved the solubility, reduced the toxicity, extended the half-life of drugs, and augmented the therapeutic window. All these results imply that H6 micelles have great potential for suppression of tumor metastasis.


Author(s):  
Yingjie Zhai ◽  
Saisai Guo ◽  
Chunhui Liu ◽  
Chunfen Yang ◽  
Jinfeng Dou ◽  
...  

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