Submicron lipid emulsion as a drug delivery system for nalbuphine and its prodrugs

Wang, Jhi Joung; Sung, K. C.; Hu, Oliver Yoa Pu; Yeh, Chia-Yi; Fang, Jia You

doi:10.1016/j.jconrel.2006.07.023

Cited by 96 publications

(53 citation statements)

References 31 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Generally, it was expected that the incorporation of DZM into nanoemulsion would enlarge the droplet size, since additional lipophilic molecules need to be solubilized in the oil phase [1]. However, the obtained results also imply a possible interaction between DZM and emulsifier layer and, consequently, partial drug localization in the o/w interface leading to the reduction of the surface tension and therefore the droplet size, during the homogenization step [11,19].…”

Section: Resultsmentioning

confidence: 91%

A full factorial design in the formulation of diazepam parenteral nanoemulsions: Physicochemical characterization and stability evaluation

Cekić¹,

Đorđević²,

Savić³

et al. 2015

Savr tehnol

View full text Add to dashboard Cite

Using the experimental design methodology, we have developed and characterized nanoemulsions for a parenteral delivery using diazepam as a model drug. The formulations containing 20 or 30% (w/w) of medium chain triglycerides or the mixture of medium chain triglycerides and soybean oil as the oil phase, soybean lecithin and polysorbate 80 as emulsifiers, and a phosphate buffer solution as the aqueous phase were prepared by cold high pressure homogenization. The obtained nanoemulsions were evaluated in terms of droplet size, size distribution, surface charge, drug-vehicle interactions and physical stability. To evaluate the effects of the oil phase type, oil content and drug presence, as well as their interactions on critical quality attributes of nanoemulsions, a three-factor two-level full factorial design was applied. After the preparation, all nanoemulsions revealed small spherical droplets in the range 170-210 nm, with the narrow droplet size distribution (< 0.15) and the surface charge about -60 mV. The experimental design results indicated that not only factors alone (oil type, oil content, presence of drug), but their interactions also had a significant effect on the nanoemulsion droplet size, polydispersity index, and zeta potential. During two months of storage at 25 °C, all nanoemulsions formulated with the medium chain triglycerides-soybean oil mixture (4:1, w/w) remained physically stable, without considerable changes in monitored parameters. Physicochemical characteristics and stability of these nanoemulsions demonstrated their suitability for parenteral drug delivery.

show abstract

Section: Resultsmentioning

confidence: 91%

A full factorial design in the formulation of diazepam parenteral nanoemulsions: Physicochemical characterization and stability evaluation

Cekić¹,

Đorđević²,

Savić³

et al. 2015

Savr tehnol

View full text Add to dashboard Cite

show abstract

“…The drug is stably retained in the lipid cores for a determined duration, followed by its slow release into the external phase. The release from the inner phase supplements the depletion of the drug from the external phase, supplying sustained and controlled delivery of the drug [23] .…”

Section: Discussionmentioning

confidence: 99%

Development and evaluation of lipid nanoparticles for camptothecin delivery: a comparison of solid lipid nanoparticles, nanostructured lipid carriers, and lipid emulsion

Huang

Hua

Yang³

et al. 2008

Acta Pharmacologica Sinica

Self Cite

177

View full text Add to dashboard Cite

Aim: Camptothecin is an anticancer drug that acts against a broad spectrum of tumors. The clinical application of camptothecin is limited by its insolubility, instability, and toxicity problems. The aim of this study was to develop and characterize lipid nanoparticles with different lipid cores which can circumvent these problems. Methods: Lipid nanoparticles made of Precirol (solid lipid nanoparticles; SLN-P), Compritol (SLN-C), Precirol+squalene (nanostructured lipid carriers; NLC), and squalene (a lipid emulsion; LE) as the lipid core material were prepared. These systems were assessed and compared by evaluating the mean diameter, surface charge, molecular environment, camptothecin release, and cell viability against a melanoma. The safety and storage stability of these systems were also preliminarily examined. Results: The particle size ranged from 190 to 310 nm, with the NLC and LE showing the smallest and largest sizes, respectively. The in vitro drug release occurred in a sustained manner in decreasing order as follows: LE>NLC>SLN-P>SLN-C. It was found that varying the type of inner phase had profound effects on cell viability. The SLN-P generally showed higher cytotoxicity than the free control. The treatment of melanomas with the camptothecin-loaded SLN-C and NLC yielded cytotoxicity comparable to that of the free form. The percentage of erythrocyte hemolysis by all nanoparticles was ≤5%, suggesting a good tolerance to lipid nanoparticles. Conclusion: The results collectively suggest that the SLN-P may have the potential to serve as a delivery system for parenteral camptothecin administration because of the sustained drug release, strong cytotoxicity, limited hemolysis, and good storage stability. Key wordscamptothecin; solid lipid nanoparticle; nanostructured lipid carrier; lipid emulsion; drug delivery; melanoma 4 Correspondence to Prof Jia-you FANG.Phn 886-3-211-8800, ext 5521.

show abstract

“…5,18 O tamanho da cadeia hidrocarbonada, bem como o grau de saturação de suas ligações afeta a capacidade de solubilização de alguns fármacos nos óleos. 3,19,20 Dessa forma, muitas vezes misturas de óleos são utilizadas para se alcançar boas solubilização e emulsificação. 15,17,21,22 Óleos biocompatíveis alternativos, como a vitamina E e seus derivados, têm sido mais recentemente investigados para a liberação de fármacos, como paclitaxel, claritromicina e outros.…”

Section: óLeounclassified

“…25 A utilização de esqualeno como fase oleosa forma nanoemulsões estáveis com pequeno diâmetro de gotícula. 19 Estudos clínicos têm sido realizados visando demonstrar a segurança do esqualeno 10 e vários outros óleos pela via parenteral, na busca de produtos estáveis e biocompatíveis.…”

Section: óLeounclassified

Nanoemulsões como sistemas de liberação parenteral de fármacos

Bruxel¹,

Laux²,

Wild³

et al. 2012

Quím. Nova

View full text Add to dashboard Cite

Recebido em 20/10/11; aceito em 29/3/12; publicado na web em 3/7/12 NANOEMULSIONS AS PARENTERAL DRUG DELIVERY SYSTEMS. Lipid nanoemulsions have recently been proposed as parenteral delivery systems for poorly-soluble drugs. These systems consist of nanoscale oil/water dispersions stabilized by an appropriate surfactant system in which the drug is incorporated into the oil core and/or adsorbed at the interface. This article reviews technological aspects of such nanosystems, including their composition, preparation methods, and physicochemical properties. From this review, it was possible to identify five groups of nanoemulsions based on their composition. Biopharmaceutical aspects of formulations containing some commercially available drugs (diazepam, propofol, dexamethasone, etomidate, flurbiprofen and prostaglandin E1) were then discussed.Keywords: emulsion; parenteral; drug. INTRODUÇÃOA solubilização de fármacos de reduzida hidrossolubilidade visando sua administração parenteral representa um grande desafio na área de desenvolvimento de medicamentos. Diversas estratégias são descritas na literatura para esta finalidade, incluindo a modificação do pH do veículo, a adição de cossolventes ou, ainda, a formação de complexos de inclusão com ciclodextrinas.1 Entretanto, limitações relacionadas à biocompatibilidade dos adjuvantes empregados, aos relatos de dor e de possível precipitação dos fármacos durante a administração podem ser considerados como fatores limitantes do uso destas abordagens. Neste contexto, sistemas nanoestruturados têm se mostrado promissores. Nanoemulsões lipídicas óleo em água têm sido empregadas há mais de 40 anos como fonte de calorias e ácidos graxos essenciais 2 e, mais recentemente, como sistemas de liberação de fármacos. A biocompatibilidade das matérias-primas empregadas para a sua obtenção (óleos de origem natural ou semissintética e fosfolipídeos) torna estes sistemas uma alternativa promissora para a administração de diversos tipos de moléculas.3 Nanoemulsões podem ser definidas como sistemas heterogêneos nos quais um líquido (a fase interna) é disperso em outro (a fase externa) na forma de gotículas, na presença de um agente emulsionante. Suas propriedades físico--químicas, influenciadas pela composição quali-e quantitativa e pelas condições de preparação, devem ser estritamente controladas, visando a administração por via parenteral e a estabilidade do sistema. 4,5 Existem na literatura algumas inconsistências relacionadas aos conceitos de nanoemulsões em relação às microemulsões. Apesar destes sistemas poderem apresentar características estruturais e visuais semelhantes em determinadas condições, diferenciam-se quanto a estabilidade termodinâmica. Contrariamente às nanoemulsões, as microemulsões são sistemas termodinamicamente estáveis. Entretanto, podem apresentar limitações para administração por via parenteral, pois suas propriedades são fortemente afetadas por alterações de temperatura e/ou diluições. Apesar da nomenclatura empregada, microemulsões apresentam geralmente tamanho...

show abstract

Submicron lipid emulsion as a drug delivery system for nalbuphine and its prodrugs

Cited by 96 publications

References 31 publications

A full factorial design in the formulation of diazepam parenteral nanoemulsions: Physicochemical characterization and stability evaluation

A full factorial design in the formulation of diazepam parenteral nanoemulsions: Physicochemical characterization and stability evaluation

Development and evaluation of lipid nanoparticles for camptothecin delivery: a comparison of solid lipid nanoparticles, nanostructured lipid carriers, and lipid emulsion

Nanoemulsões como sistemas de liberação parenteral de fármacos

Contact Info

Product

Resources

About