Polymeric Micelles, a Promising Drug Delivery System to Enhance Bioavailability of Poorly Water-Soluble Drugs

Xu, Wei; Ling, Peixue; Tian-min, Zhang

doi:10.1155/2013/340315

Cited by 466 publications

(225 citation statements)

References 175 publications

(193 reference statements)

Supporting

Mentioning

223

Contrasting

Order By: Relevance

“…Study design of animal work. DOI: 10.3109/10717544.2015.1110846 (on day 3.5) by administering the microcapsules orally (Xu et al, 2013), with blood collection at various time points over a period of 10 hours.…”

Section: Experimental Protocolmentioning

confidence: 99%

A comprehensive study of novel microcapsules incorporating gliclazide and a permeation enhancing bile acid: hypoglycemic effect in an animal model of Type-1 diabetes

et al. 2015

View full text Add to dashboard Cite

Context: Gliclazide (G) is a commonly prescribed drug for Type 2 diabetes (T2D). In a recent study, we found that when G was combined with a primary bile acid, and gavaged to an animal model of Type 1 diabetes (T1D), it exerted a hypoglycemic effect. We hypothesized this to be due to metabolic activation of the primary bile acid into a secondary or a tertiary bile acid, which enhanced G solubility and absorption. The tertiary bile acid, taurocholic acid (TCA), has shown strong permeation-enhancing effects in vivo. Thus, we aimed to design, characterize, and test microcapsules incorporating G and TCA in an animal model of T1D. Methods: Microcapsules were prepared using the polymer sodium alginate (SA). G-SA microcapsules (control) and G-TCA-SA microcapsules (test) were extensively examined (in-vitro) at different pH and temperatures. The microcapsules were gavaged to diabetic rats, and blood glucose and G concentrations in serum were examined. Ex-vivo studies were also performed using a muscle cell line (C2C12), and cell viability and glucose intake post-treatment were examined. Results: G-TCA-SA microcapsules showed good stability, uniformity, and thermal and chemical excipient compatibilities. TCA did not change the size or the shape of the microcapsules, but it enhanced their mechanical resistance and reduced their swelling properties. G-TCA-SA enhanced the viability of C2C12 cells over 24 hours, and exerted a hypoglycemic effect in alloxan-induced type-1 diabetic rats. Conclusions: The incorporation of TCA into G-microcapsules resulted in functionally improved microcapsules with a positive effect on cell viability and glycemic control in Type-1 diabetic animals.

show abstract

Section: Experimental Protocolmentioning

confidence: 99%

A comprehensive study of novel microcapsules incorporating gliclazide and a permeation enhancing bile acid: hypoglycemic effect in an animal model of Type-1 diabetes

et al. 2015

View full text Add to dashboard Cite

show abstract

“…Micelles are formed in aqueous solutions when the concentration of the block copolymer increases above a certain concentration or critical micelle concentration (Xu, Ling, Zhang, 2013).…”

Section: Polymeric Micellesmentioning

confidence: 99%

A review of nanotechnology with an emphasis on Nanoplex

Kadam

Shendge

Pande

2015

Braz. J. Pharm. Sci.

View full text Add to dashboard Cite

The use of nanotechnology based on the development and fabrication of nanostructures is one approach that has been employed to overcome the challenges involved with conventional drug delivery systems. Formulating Nanoplex is the new trend in nanotechnology. A nanoplex is a complex formed by a drug nanoparticle with an oppositely charged polyelectrolyte. Both cationic and anionic drugs form complexes with oppositely charged polyelectrolytes. Compared with other nanostructures, the yield of Nanoplex is greater and the complexation efficiency is better. Nanoplex are also easier to prepare. Nanoplex formulation is characterized through the production yield, complexation efficiency, drug loading, particle size and zeta potential using scanning electron microscopy, differential scanning calorimetry, X-ray diffraction and dialysis studies. Nanoplex have wide-ranging applications in different fields such as cancer therapy, gene drug delivery, drug delivery to the brain and protein and peptide drug delivery.Uniterms: Nanotechnology. Nanoplex/formulation. Nanoplex/characterization. Nanoplex/applications O uso da nanotecnologia baseada no desenvolvimento e na fabricação de nanoestruturas é uma abordagem que tem sido empregada para superar os desafios envolvidos nos sistemas de liberação de fármacos convencionais. A formulação de nanoplexos é a nova tendência na nanotecnologia. Um nanoplexo é um complexo formado pela nanopartícula do fármaco com poplieletrólito de carga oposta. Tanto fármacos catiônicos quanto aniônicos formam complexos com polieletrólitos opostamente carregados. Comparado com outras nanoestruturas, o rendimento dos nanoplexos é maior e a eficiência de complexação é melhor. Nanoplexos são, também. De mais fácil preparação. A formulação de nanoplexo é caracterizada pelo rendimento de produção, eficiência de complexação, carga do fármaco, tamanho de partícula e potencial zeta, utilizando microscopia eletrônica de varredura, calorimetria exploratória diferencial, difração de raios X e estudos de diálise. Os nanoplexos têm aplicações amplas em diferentes campos, como terapia antineoplásica, liberação em terapia gênica, liberação cerebral de fármaco, liberação de fármacos protéicos e peptídicos.Unitermos: Nanotecnologia. Nanoplexos/formulação. Nanoplexos/caracterização. Nanoplexos/ aplicações.

show abstract

“…Nanosized materials in form of nanoparticles, micelles and liposomes are among the most promising drug delivery systems for the transport of pharmaceuticals to the site of action, reducing toxicity and side effects associated to several drugs [3,4]. In particular, nanocarriers with appropriate physicochemical characteristics such as dimensions and surface charge have been recently investigated as delivery systems able to protect drugs from enzymatic degradation, improve drug pharmacokinetics and enter cells and various cellular compartments [5][6][7].…”

Section: Introductionmentioning

confidence: 99%

Analysis of Operating Conditions Influencing the Morphology and In vitro Behaviour of Chitosan Coated Liposomes

Venturini¹

2014

J Nanomed Nanotechnol

View full text Add to dashboard Cite

Among nanoparticle-based drug delivery formulations, lecithin/chitosan liposomes are promising candidates because of their biocompatibility, biodegradability and bioadhesion properties. Lecithin is a mixture of highly biocompatible phospholipids, while chitosan represents one of the most used polymers in pharmaceutical formulations. Their combination results in positively charged complexes that are able to sustain a specific, prolonged and controlled release. Scarce reproducibility and batch-to-batch variation in lecithin/chitosan liposome synthesis, as well as difficult scale-up to industrial production, is a major challenge for their utilization. Here we present a strictly controlled procedure, based on ethanol diffusion in water, which yields to a precise and reproducible self-organization of lecithin and chitosan molecules. We analysed the size, surface charge and stability of chitosan coated liposomes at different lecithin/ chitosan ratios. We found that increasing the lecithin/chitosan ratio both mean particle size and surface charge were progressively reduced. A good stability was observed for all formulations, though interactions occurred in liposomes with low amount of surface-adsorbed chitosan. Chitosan coated liposomes interact with A549 and Caco-2 cells inducing low toxic effects only with prolonged incubation times. In conclusion, the proposed procedure provides good reproducibility in the formation of non-toxic and highly stable formulations of chitosan coated liposomes as drug delivery systems.as lecithin, spontaneously forming supramolecular aggregates [21]. The appropriate combination of lecithin with chitosan results in positively charged complexes with specific, prolonged and controlled release characteristics. Several authors have described the use of chitosan as a coating material for liposomes, resulting in formulation with an improved oral bioavailability for peptide and protein drugs [22][23][24][25]. Chitosan-coated liposomes (CCL) containing insulin have been shown to produce hypoglycaemic effects in mice after oral administration [26]. Moreover, lecithin-chitosan nanoparticles can strongly interact with mammalian skin, which is slightly negatively charged, offering a better topical delivery of active compounds [27,28]. On the contrary, in conventional uncoated liposomes without any surface modification, the lack of positive charges does not ensure close contact between nanoparticles and skin. As a consequence, uncoated liposomes are rapidly removed from skin surface.These findings suggest that CCL possess a great potential as drug delivery systems improving the permeation of entrapped drugs across various biological barriers including skin and mucosal tissue [23,[29][30][31].

show abstract

Polymeric Micelles, a Promising Drug Delivery System to Enhance Bioavailability of Poorly Water-Soluble Drugs

Cited by 466 publications

References 175 publications

A comprehensive study of novel microcapsules incorporating gliclazide and a permeation enhancing bile acid: hypoglycemic effect in an animal model of Type-1 diabetes

A comprehensive study of novel microcapsules incorporating gliclazide and a permeation enhancing bile acid: hypoglycemic effect in an animal model of Type-1 diabetes

A review of nanotechnology with an emphasis on Nanoplex

Analysis of Operating Conditions Influencing the Morphology and In vitro Behaviour of Chitosan Coated Liposomes

Contact Info

Product

Resources

About