scholarly journals Enhanced Oral Absorption of Icaritin by Using Mixed Polymeric Micelles Prepared with a Creative Acid-Base Shift Method

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3450
Author(s):  
Cheng Tang ◽  
Xiaoming Chen ◽  
Hua Yao ◽  
Haiyan Yin ◽  
Xiaoping Ma ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
In Vitro Release ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
Acid Base ◽  
High Drug ◽  
Mixed Polymeric Micelles ◽  
High Drug Loading

The purpose of this study was to develop mixed polymeric micelles with high drug loading capacity to improve the oral bioavailability of icaritin with Soluplus® and Poloxamer 407 using a creative acid-base shift (ABS) method, which exhibits the advantages of exclusion of organic solvents, high drug loading and ease of scaling-up. The feasibility of the ABS method was successfully demonstrated by studies of icaritin-loaded polymeric micelles (IPMs). The prepared IPMs were characterized to have a spherical shape with a size of 72.74 ± 0.51 nm, and 13.18% drug loading content. In vitro release tests confirmed the faster release of icaritin from IPMs compared to an oil suspension. Furthermore, bioavailability of icaritin in IPMs in beagle dogs displayed a 14.9-fold increase when compared with the oil suspension. Transcellular transport studies of IPMs across Caco-2 cell monolayers confirmed that the IPMs were endocytosed in their intact forms through macropinocytosis, clathrin-, and caveolae-mediated pathways. In conclusion, the results suggested that the mixed micelles of Soluplus® and Poloxamer 407 could be a feasible drug delivery system to enhance oral bioavailability of icaritin, and the ABS method might be a promising technology for the preparation of polymeric micelles to encapsulate poorly water-soluble weakly acidic and alkaline drugs.

Co-delivery of dual chemo-drugs with precisely controlled, high drug loading polymeric micelles for synergistic anti-cancer therapy

2020 ◽  
Vol 8 (3) ◽  
pp. 949-959 ◽  
Author(s):  
Yuchen Wu ◽  
Shixian Lv ◽  
Yongjuan Li ◽  
Hua He ◽  
Yong Ji ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
High Drug ◽  
Delivery Strategy ◽  
Anti Cancer ◽  
High Drug Loading

The introduction of donor-receptor coordination between micelles and drug payloads provides a precise co-delivery strategy for two different chemo-drugs with high drug loading and ROS responsiveness.

Water soluble multiarm-polyethylene glycol–betulinic acid prodrugs: design, synthesis, and in vivo effectiveness

2014 ◽  
Vol 5 (19) ◽  
pp. 5775-5783 ◽  
Author(s):  
Lin Dai ◽  
Dan Li ◽  
Jing Cheng ◽  
Jing Liu ◽  
Li-Hong Deng ◽  
...  
Keyword(s):  
Polyethylene Glycol ◽  
Betulinic Acid ◽  
Water Solubility ◽  
Drug Loading ◽  
Water Soluble ◽  
Loading Capacity ◽  
Design Synthesis ◽  
High Drug ◽  
High Drug Loading

Multiarm-polyethylene glycol–betulinic acid prodrugs were prepared by using multiarm-polyethylene glycol linkers and betulinic acid, which exhibited high drug loading capacity, good water solubility, and excellent anticancer activity.

scholarly journals High-drug-loading capacity of redox-activated biodegradable nanoplatform for active targeted delivery of chemotherapeutic drugs

2020 ◽  
Vol 7 (4) ◽  
pp. 359-369
Author(s):  
Hai Zhang ◽  
Jianqin Yan ◽  
Heng Mei ◽  
Shengsheng Cai ◽  
Sai Li ◽  
...  
Keyword(s):  
Drug Release ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Active Targeting ◽  
Control Group ◽  
Loading Capacity ◽  
Disulfide Linkage ◽  
High Drug ◽  
High Drug Loading

Abstract Challenges associated with low-drug-loading capacity, lack of active targeting of tumor cells and unspecific drug release of nanocarriers synchronously plague the success of cancer therapy. Herein, we constructed active-targeting, redox-activated polymeric micelles (HPGssML) self-assembled aptamer-decorated, amphiphilic biodegradable poly (benzyl malolactonate-co-ε-caprolactone) copolymer with disulfide linkage and π-conjugated moieties. HPGssML with a homogenous spherical shape and nanosized diameter (∼150 nm) formed a low critical micellar concentration (10−3 mg/mL), suggesting good stability of polymeric micelles. The anticancer drug, doxorubicin (DOX), can be efficiently loaded into the core of micelles with high-drug-loading content via strong π–π interaction, which was verified by a decrease in fluorescence intensity and redshift in UV adsorption of DOX in micelles. The redox sensitivity of polymeric micelles was confirmed by size change and in vitro drug release in a reducing environment. Confocal microscopy and flow cytometry assay demonstrated that conjugating aptamers could enhance specific uptake of HPGssML by cancer cells. An in vitro cytotoxicity study showed that the half-maximal inhibitory concentration (IC50) of DOX-loaded HPGssML was two times lower than that of the control group, demonstrating improved antitumor efficacy. Therefore, the multifunctional biodegradable polymeric micelles can be exploited as a desirable drug carrier for effective cancer treatment.

Enhancing tablet disintegration characteristics of a highly water-soluble high-drug-loading formulation by granulation process

2016 ◽  
Vol 23 (6) ◽  
pp. 587-595 ◽  
Author(s):  
Preetanshu Pandey ◽  
Christopher Levins ◽  
Steve Pafiakis ◽  
Brian Zacour ◽  
Dilbir S. Bindra ◽  
...  
Keyword(s):  
Drug Loading ◽  
Water Soluble ◽  
Granulation Process ◽  
High Drug ◽  
Tablet Disintegration ◽  
High Drug Loading

Tocophersolan stabilized lipid nanocapsules with high drug loading to improve the permeability and oral bioavailability of curcumin

2019 ◽  
Vol 560 ◽  
pp. 219-227 ◽  
Author(s):  
Pradnya Bapat ◽  
Rohan Ghadi ◽  
Dasharath Chaudhari ◽  
Sameer S. Katiyar ◽  
Sanyog Jain
Keyword(s):  
Oral Bioavailability ◽  
Drug Loading ◽  
Lipid Nanocapsules ◽  
High Drug ◽  
High Drug Loading

scholarly journals Synthesis of high drug loading, reactive oxygen species and esterase dual-responsive polymeric micelles for drug delivery

RSC Advances ◽  
2019 ◽  
Vol 9 (5) ◽  
pp. 2371-2378 ◽  
Author(s):  
Nan Wang ◽  
Xiao-Chuan Chen ◽  
Ruo-Lin Ding ◽  
Xian-Ling Yang ◽  
Jun Li ◽  
...  
Keyword(s):  
Reactive Oxygen Species ◽  
Drug Delivery ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Oxygen Species ◽  
High Drug ◽  
Dual Responsive ◽  
Release Drug ◽  
Stimulus Responsive ◽  
High Drug Loading

A novel high drug loading, controlled-release drug delivery system was constructed with dual-stimulus responsive abilities in cells.

High Drug Loading and Sub-Quantitative Loading Efficiency of Polymeric Micelles Driven by Donor–Receptor Coordination Interactions

2018 ◽  
Vol 140 (4) ◽  
pp. 1235-1238 ◽  
Author(s):  
Shixian Lv ◽  
Yuchen Wu ◽  
Kaimin Cai ◽  
Hua He ◽  
Yongjuan Li ◽  
...  
Keyword(s):  
Polymeric Micelles ◽  
Drug Loading ◽  
High Drug ◽  
Loading Efficiency ◽  
High Drug Loading

Enhanced oral bioavailability of a cancer preventive agent (SR13668) by employing polymeric nanoparticles with high drug loading

2012 ◽  
Vol 101 (10) ◽  
pp. 3877-3885 ◽  
Author(s):  
Hao Shen ◽  
Aryamitra A. Banerjee ◽  
Paulina Mlynarska ◽  
Mathew Hautman ◽  
Seungpyo Hong ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Polymeric Nanoparticles ◽  
Drug Loading ◽  
High Drug ◽  
High Drug Loading
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