Approaches for the development of solid and semi-solid lipid-based formulations

Jannin, Vincent; Musakhanian, Jasmine; Marchaud, Delphine

doi:10.1016/j.addr.2007.09.006

Cited by 319 publications

(189 citation statements)

References 114 publications

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“…Differential scanning calorimetry can be described as a thermal analysis technique used in the investigation of melting, crystallization, solid-to-solid transition temperatures of lipids, and determination of the solid fat content of the excipient (Jannin et al, 2008). It enables the measurement of temperature change and heat flow which occurs when a material undergoes phase transition.…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

“…This problem can be rectified by addition of longer chain triglycerides to speed up nucleation and crystallization of trilaurin or other resembling glycerides (Bunjes et al, 1996). During the course of production and storage glycerides may exist under various polymorphic forms such as hexagonal (α), orthorhombic (β´), and triclinic (β), which can be confirmed by X-ray diffraction (Jannin et al, 2008). Polymorphic changes depend on the thermal history of the lipid (Jannin et al, 2008).…”

Section: Triglyceridesmentioning

confidence: 99%

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Solid lipid nanoparticles for ocular drug delivery

2010

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Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

Section: Triglyceridesmentioning

confidence: 99%

Solid lipid nanoparticles for ocular drug delivery

2010

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“…The lipid droplets formed upon dispersion of self-emulsifying LBDDS may directly facilitate drug absorption, regardless of the bile salt-mediated mixed micelle transport system. Other mechanisms proposed include protection of the drug inside the lipid droplets from chemical and enzymatic degradation, localized in the aqueous environment, changes in gastrointestinal membrane permeability, and promo-tion of lymphatic drug transport (10,13). Strategies for increasing the absorption of hydrophobic drugs with LBDDS are presented in Table III.…”

Section: Strategies To Enhance the Bioavailability Of Orally Administmentioning

confidence: 99%

“…Due to composition diversity, formulations belonging to different classes according to LFCS behave differently in the GIT. Type III and IV formulations may, for example, lose their sol- vent capacity on dispersion due to diffusion of water-soluble components into the bulk aqueous phase, leading to drug precipitation (13,16,17). Digestion of some formulation components in the GIT can also contribute to decreased solvent capacity.…”

Section: Strategies To Enhance the Bioavailability Of Orally Administmentioning

confidence: 99%

Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

Čerpnjak¹,

Zvonar²,

Gašperlin³

et al. 2013

Acta Pharmaceutica

186

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Low oral bioavailability as a consequence of low water solubility of drugs is a growing challenge to the development of new pharmaceutical products. One of the most popular approaches of oral bioavailability and solubility enhancement is the utilization of lipid-based drug delivery systems. Their use in product development is growing due to the versatility of pharmaceutical lipid excipients and drug formulations, and their compatibility with liquid, semi-solid, and solid dosage forms. Lipid formulations, such as self-emulsifying (SEDDS), self-microemulsifying SMEDDS) and self--nanoemulsifying drug delivery systems (SNEDDS) were explored in many studies as an efficient approach for improving the bioavailability and dissolution rate of poorly water-soluble drugs. One of the greatest advantages of incorporating poorly soluble drugs into such formulations is their spontaneous emulsification and formation of an emulsion, microemulsion or nanoemulsion in aqueous media. This review article focuses on the following topics. First, it presents a classification overview of lipid-based drug delivery systems and mechanisms involved in improving the solubility and bioavailability of poorly water-soluble drugs. Second, the article reviews components of lipid-based drug delivery systems for oral use with their characteristics. Third, it brings a detailed description of SEDDS, SMEDDS and SNEDDS, which are very often misused in literature, with special emphasis on the comparison between microemulsions and nanoemulsions.Keywords: lipid-based drug delivery systems (LBDDS), self-emulsifying drug delivery systems (SEDDS), self--microemulsifying drug delivery systems (SMEDDS), self-nanoemulsifying drug delivery systems (SNEDDS), microemulsions, nanoemulsions

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“…In an attempt to combine the advantages of SMEFs with those of solid dosage forms and overcome the shortcomings of liquid formulations, increasing attention has been focused on solid self-(micro) emulsifying formulations. The thermotropic stability of SMEFs and their high drug loading efficiency make them a promising system for low aqueous soluble drugs (Jannin et al, 2007). SMEFs are usually placed in soft gelatin capsules, but can also be transformed into granules, pellets, powders for dry filled capsules or tablet preparations (Nazzal, Khan, 2006;Serratoni, Newton, 2007;Abdalla et al, 2008;Tan et al, 2009).…”

Section: Self-microemulsifying Formulationsmentioning

confidence: 99%

Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs

Wadhwa¹,

Nair²,

Kumria³

2011

Braz. J. Pharm. Sci.

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Self-emulsifying therapeutic system (SETs) provide an effective and intelligent solution to the various issues related to the formulation of hydrophobic drugs with limited solubility in gastrointestinal fluid. Although the potential utility of SETs is well known, only in recent years has a mechanistic understanding of the impact of these systems on drug disposition emerged. These in situ emulsion-forming systems have a high stability when incorporated in various dosage forms. SETs are being looked upon as systems which can overcome the problems associated with delivery of poorly water soluble drugs. An in-depth knowledge about lipids and surfactants that can contribute to these systems, criterion for their selection and the proportion in which they can be used, represent some crucial factors determining the in vivo performance of these systems. This article presents a comprehensive account of various types of self-emulsifying formulations with emphasis on their composition and examples of currently marketed preparations.Uniterms: Lipid based formulations. Self-emulsifying therapeutic system. Self-emulsification.O sistema terapêutico auto-emulsionante (SETs) fornece solução eficaz e inteligente para os vários problemas relativos à formulação de fármacos hidrofóbicos com solubilidade limitada no fluido gastrintestinal. Embora a utilidade potencial dos SETs seja bem conhecida, só recentemente se compreendeu, mecanisticamente,o impacto desses sistemas na disposição de fármacos. Estes sistemas de formação de emulsão in situ têm alta estabilidade, quando incorporados em várias formas de dosagem. Os SETs têm sido considerados como sistemas que podem resolver problemas associados à liberação de fármacos pouco solúveis em água. O conhecimento profundo dos lipídios e tensoativos que podem ser utilizados para estes sistemas e o critério para a sua seleção e proporção na qual eles são utilizados são alguns dos fatores cruciais que determinam o desempenho do sistema in vivo. Este artigo apresenta o relato abrangente de vários tipos de formulações auto-emulsificantes, com ênfase em sua composição e exemplos das preparações que são correntemente comercializadas.Unitermos: Formulações baseadas em lipídio. Sistema terapêutico auto-emulsificante. Autoemulsificação.

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Approaches for the development of solid and semi-solid lipid-based formulations

Cited by 319 publications

References 114 publications

Solid lipid nanoparticles for ocular drug delivery

Solid lipid nanoparticles for ocular drug delivery

Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs

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