Development of topotecan loaded lipid nanoparticles for chemical stabilization and prolonged release

Souza, Leonardo Gomes de; Silva, E.J.; Martins, André; Mota, Mariana Flávia da; Braga, Rodolpho C.; Lima, Eliana Martins; Valadares, Marize Campos; Taveira, Stephânia Fleury; Marreto, Ricardo Neves

doi:10.1016/j.ejpb.2011.02.012

Cited by 130 publications

(77 citation statements)

References 32 publications

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“…The dispersion had a total lipid content of 2% (w/v), stabilized by 1.25% (w/v) of surfactant (lecithin: taurodeoxycholate, 4:1 ratio). The stearic acid: oleic acid ratio in the NLCs was 3:1 (Souza et al, 2011). The CP in the formulation comprised 4% (w/w) of the lipid content.…”

Section: Production and Characterization Of Cp-loaded Nlcsmentioning

confidence: 99%

“…NLCs have attracted researchers' attention due to their small size, high drug loading, and biocompatible and biodegradable lipid composition. NLCs were produced in this case using a simple microemulsion technique, which was previously employed by our research group to produce lipid nanoparticles containing the cytotoxic drug topotecan (Souza et al, 2011). It is important to note that several papers have reported that NLCs have enormous potential to improve skin penetration and the retention of drugs in the skin (Pardeike, Homoss, Muller, 2009).…”

Section: Introductionmentioning

confidence: 99%

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In vitro skin penetration of clobetasol from lipid nanoparticles: drug extraction and quantitation in different skin layers

Silva

Taveira

Lima

et al. 2012

Braz. J. Pharm. Sci.

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Clobetasol propionate (CP) is a potent topical corticosteroid that causes several cutaneous and systemic side effects. In the present work, CP was encapsulated in nanostructured lipid carriers (NLCs) to increase drug retention in the outer skin layers and improve the safety of topical therapy. NLCs were prepared using a microemulsion technique with a mixture of lecithin, taurodeoxycholate, stearic acid, and oleic acid. In vitro penetration studies were performed in a modified Franz-type diffusion cell, and porcine ears were used as a model of human skin. A simple and sensitive liquid chromatographic method was developed and validated for clobetasol determination in different skin layers. NLCs presented uniform size distribution, high zeta potentialand entrapment efficiency values (> 98%). The analytical procedure was validated according to FDA guidelines. Clobetasol recoveries from skin samples were higher than 85%, with no interference of skin components and NLC ingredients. In experiments, after 6 h, a higher drug accumulation in the stratum corneum arising from NLCs compared to aqueous CP solution was observed. Thus, the NLCs demonstrated high potential for targeting CP to the skin and ensuring drug accumulation in the stratum corneum.Uniterms: Clobetasol propionate/in vitro skin penetration. Nanostructured lipid carriers/in vitro study.Proprionato de clobetasol (CP) é um potente corticóide tópico, que apresenta vários efeitos adversos cutâneos e sistêmicos. No presente trabalho, CP foi encapsulado em carreadores lipídicos nanoestruturados (NLCs) visando aumentar a retenção do fármaco nas camadas superficiais da pele e a segurança da terapia tópica. NLCs foram preparados usando a técnica de diluição de microemulsão com mistura de lecitina, taurodesoxicolato, ácido esteárico e ácido oléico. Estudos de penetração in vitro foram realizados em células de difusão de Franz modificadas usando pele de orelha de porco como modelo de pele humana. Um método simples e sensível de cromatografia líquida foi desenvolvido e validado para a determinação de clobetasol nas diferentes camadas da pele. NLCs apresentaram distribuição de tamanho uniforme e valores elevados de potencial zeta e eficiência de encapsulação (>98%). O procedimento analítico foi validado de acordo com as diretrizes do FDA. A recuperação de clobetasol a partir das amostras de pele foi maior que 85%, sem interferência dos componentes da pele e dos excipientes das NLCs. Após 6 horas de experimento observou-se maior acúmulo do fármaco a partir das NLCs comparado à solução aquosa de CP. Dessa forma, as NLCs mostraram elevado potencial para direcionar o CP para a pele, pois elas possibilitaram o acúmulo do fármaco no estrato córneo. Unitermos: Proprionato de clobetasol/penetração cutânea in vitro. Carreadores lipídicos nanoestruturados/ estudo in vitro.

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Section: Production and Characterization Of Cp-loaded Nlcsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

In vitro skin penetration of clobetasol from lipid nanoparticles: drug extraction and quantitation in different skin layers

Silva

Taveira

Lima

et al. 2012

Braz. J. Pharm. Sci.

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“…The reduction in SLN size, however, was not statistically significant. 46 Tryptanthrin, an ancient traditional folk medicine, was shown to be useful in treating certain cancers, in particular those that exhibit multidrug resistance. However, since tryptanthrin is insoluble in most biocompatible solvents, delivering it into cancer cells is challenging when using conventional administration techniques, such as oral, intravenous or intramuscular delivery routes.…”

Section: Impact Of Variables On Size Of Slns and Nlcsmentioning

confidence: 99%

The Impact of Variables on Particle Size of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers; A Comparative Literature Review

Bahari¹,

Hamishehkar²

2016

Adv Pharm Bull

180

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“…However, the high amount of Cremophor EL results in significant side effects, which limits the clinical application of PTX. Although various approaches were employed to enhance the aqueous solubility of PTX by utilizing liposomes, micelles, nanoparticles, and liquid crystalline nanoparticles, 30 each approach suffers from known limitations. Still, few publications have reported on the co-delivery of genes and PTX for use as a type of lung cancer therapy.…”

Section: Introductionmentioning

confidence: 99%

Targeted lung cancer therapy: preparation and optimization of transferrin-decorated nanostructured lipid carriers as novel nanomedicine for co-delivery of anticancer drugs and DNA

Shao¹,

Shao²,

Tan³

et al. 2015

IJN

122

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Purpose Nanostructured lipid carriers (NLC) represent an improved generation of lipid nanoparticles. They have specific nanostructures to accommodate drugs/genes, and thus achieve higher loading capacity. The aim of this study was to develop transferrin (Tf)-decorated NLC as multifunctional nanomedicine for co-delivery of paclitaxel (PTX) and enhanced green fluorescence protein plasmid. Methods Firstly, Tf-conjugated ligands were synthesized. Secondly, PTX- and DNA-loaded NLC (PTX-DNA-NLC) was prepared. Finally, Tf-containing ligands were used for the surface decoration of NLC. Their average size, zeta potential, drug, and gene loading were evaluated. Human non-small cell lung carcinoma cell line (NCl-H460 cells) was used for the testing of in vitro transfection efficiency, and in vivo transfection efficiency of NLC was evaluated on mice bearing NCl-H460 cells. Results Tf-decorated PTX and DNA co-encapsulated NLC (Tf-PTX-DNA-NLC) were nano-sized particles with positive zeta potential. Tf-PTX-DNA-NLC displayed low cytotoxicity, high gene transfection efficiency, and enhanced antitumor activity in vitro and in vivo. Conclusion The results demonstrated that Tf-PTX-DNA-NLC can achieve impressive antitumor activity and gene transfection efficiency. Tf decoration also enhanced the active targeting ability of the carriers to NCl-H460 cells. The novel drug and gene delivery system offers a promising strategy for the treatment of lung cancer.

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Development of topotecan loaded lipid nanoparticles for chemical stabilization and prolonged release

Cited by 130 publications

References 32 publications

In vitro skin penetration of clobetasol from lipid nanoparticles: drug extraction and quantitation in different skin layers

In vitro skin penetration of clobetasol from lipid nanoparticles: drug extraction and quantitation in different skin layers

The Impact of Variables on Particle Size of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers; A Comparative Literature Review

Targeted lung cancer therapy: preparation and optimization of transferrin-decorated nanostructured lipid carriers as novel nanomedicine for co-delivery of anticancer drugs and DNA

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