scholarly journals Honokiol/Magnolol-Loaded Self-Assembling Lecithin-Based Mixed Polymeric Micelles (lbMPMs) for Improving Solubility to Enhance Oral Bioavailability

2021 ◽  
Vol Volume 16 ◽  
pp. 651-665
Author(s):  
Hong-Liang Lin ◽  
Wen-Ting Cheng ◽  
Ling-Chun Chen ◽  
Hsiu-O Ho ◽  
Shyr-Yi Lin ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Polymeric Micelles ◽  
Self Assembling ◽  
Mixed Polymeric Micelles

Improved oral bioavailability and anti-chronic renal failure activity of chrysophanol via mixed polymeric micelles

2020 ◽  
Vol 38 (1) ◽  
pp. 47-60
Author(s):  
Mingjia Gu ◽  
Lidan Lu ◽  
Qingxue Wei ◽  
Zhiwei Miao ◽  
Hang Zhang ◽  
...  
Keyword(s):  
Renal Failure ◽  
Chronic Renal Failure ◽  
Oral Bioavailability ◽  
Polymeric Micelles ◽  
Mixed Polymeric Micelles

Enhanced oral bioavailability of capsaicin in mixed polymeric micelles: Preparation, in vitro and in vivo evaluation

2014 ◽  
Vol 8 ◽  
pp. 358-366 ◽  
Author(s):  
Yuan Zhu ◽  
Wei Peng ◽  
Jiajia Zhang ◽  
Miaomiao Wang ◽  
Caleb Kesse Firempong ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Polymeric Micelles ◽  
In Vivo Evaluation ◽  
Mixed Polymeric Micelles

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.

scholarly journals Polymeric Micelles for the Enhanced Deposition of Hydrophobic Drugs into Ocular Tissues, without Plasma Exposure

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 744
Author(s):  
Ijeoma F. Uchegbu ◽  
Jan Breznikar ◽  
Alessandra Zaffalon ◽  
Uche Odunze ◽  
Andreas G. Schätzlein
Keyword(s):  
Polymeric Micelles ◽  
Rabbit Model ◽  
Penetration Enhancer ◽  
Hydrophobic Drugs ◽  
Ocular Tissues ◽  
Ocular Penetration ◽  
Self Assembling ◽  
Similar Dose ◽  
Oil In Water ◽  
The Stability

Commercial topical ocular formulations for hydrophobic actives rely on the use of suspensions or oil in water emulsions and neither of these formulation modalities adequately promote drug penetration into ocular tissues. Using the ocular relevant hydrophobic drug, cyclosporine A (CsA), a non-irritant ocular penetration enhancer is showcased, which may be used for the formulation of hydrophobic actives. The activity of this penetration enhancer is demonstrated in a healthy rabbit model. The Molecular Envelope Technology (MET) polymer (N-palmitoyl-N-monomethyl-N,N-dimethyl-N,N,N-trimethyl-6-O-glycolchitosan), a self-assembling, micelle-forming polymer, was used to formulate CsA into sterile filtered nanoparticulate eye drop formulations and the stability of the formulation tested. Healthy rabbits were dosed with a single dose of a MET–CsA (NM133) 0.05% formulation and ocular tissues analyzed. Optically clear NM133 formulations were prepared containing between 0.01–0.1% w/v CsA and 0.375–0.75% w/v MET polymer. NM133 0.01%, NM133 0.02% and NM133 0.05% were stable for 28 days when stored at refrigeration temperature (5–6 °C) and room temperature (16–23 °C), but there was evidence of evaporation of the formulation at 40 °C. There was no change in drug content when NM133 0.05% was stored for 387 days at 4 °C. On topical dosing to rabbits, corneal, conjunctival and scleral AUC0–24 levels were 25,780 ng.h g−1, 12,046 ng.h g−1 and 5879 ng.h g−1, respectively, with NM133 0.05%. Meanwhile, a similar dose of Restasis 0.05% yielded lower values of 4726 ng.h/g, 4813 ng.h/g and 1729 ng.h/g for the drug corneal, conjunctival and scleral levels, respectively. NM133 thus delivered up to five times more CsA to the ocular surface tissues when compared to Restasis. The MET polymer was non-irritant up to a concentration of 4% w/v. The MET polymer is a non-irritant ocular penetration enhancer that may be used to deliver hydrophobic drugs in optically clear topical ocular formulations.

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