Surfactant-mediated dissolution: Contributions of solubility enhancement and relatively low micelle diffusivity

Balakrishnan, Anand; Rege, Bhagwant D.; Amidon, Gordon L.; Polli, James E.

doi:10.1002/jps.20118

Cited by 127 publications

(98 citation statements)

References 34 publications

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“…In these drugs, dissolution of the drug is the rate limiting step in the absorption process. To triumph over these obstacles, numbers of formulation approaches are reported including the use of surfactants (Allaboun et al, 2003;Balakrishnan et al, 2004;Chakraborty et al, 2009), lipids (Yeap et al, 2013), permeation enhancers (Burcin et al, 2010;Beg et al, 2011), formation of salt (Li et al, 2005;Serajuddin, 2007), co-crystallization (Shan & Zaworotko, 2008;Qiao et al, 2011;Chadha et al, 2012), solid dispersions (Serajuddin, 1999), inclusion complexes with cyclodextrins and modified cyclodextrins (Miyake et al, 2000;Veiga et al, 2000;Wang et al, 2000;Bannwart et al, 2001;Carrier et al, 2007;Gamsiz et al, 2010a,b;Gamsiz et al, 2011;Badr-Eldin et al, 2008;Kumar et al, 2013), nanosuspensions (Patravale et al, 2004), and colloidal vesicles like liposomes (Nazzal et al, 2002a;Manconi et al, 2013;Yang et al, 2013), and niosomes (Khazaeli et al, 2007;Bayindir & Yuksel, 2010;SezginBayindir et al, 2013;Jin et al, 2013) In modern years, self-nanoemulsifying drug delivery systems (SNEDDS) are the most popular and commercially feasible lipid-based formulation approach for improving oral bioavailability of poorly water soluble and lipophilic drugs (Pouton, 2006;Date, 2007;Shweta et al, 2011). SNEDDS are precisely defined as an isotropic multi-component drug delivery systems composed of a synthetic or natural oil, surfactant, and co-surfactant that have a unique ability of forming fine oil in water micro-or nano-emulsion upon mild agitation followed by dilutio...…”

Section: Introductionmentioning

confidence: 99%

Solid self-nanoemulsifying drug delivery system (S-SNEDDS) for oral delivery of glimepiride: development and antidiabetic activity in albino rabbits

Mohd¹,

Sanka²,

Bandi³

et al. 2014

Drug Delivery

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(2015) Solid self-nanoemulsifying drug delivery system (S-SNEDDS) for oral delivery of glimepiride: development and antidiabetic activity in albino rabbits, Drug Delivery, 22:4, 499-508, DOI: 10.3109/10717544.2013 Context: This study presents novel self-nanoemulsifying drug delivery system potential of oral delivering which leads poorly aqueous soluble drug glimepiride.Objective: The objective of this study was to prepare solid self-nanoemulsifying drug delivery system (S-SNEDDS) for the improved oral delivery of glimepiride and to evaluate its therapeutic efficacy in albino rabbits.Results and discussion: The droplet size analyses revealed a droplet size of less than 200 nm. The solid state characterization of S-SNEDDS by scanning electron microscopy (SEM), X-ray powder diffraction and differential scanning calorimetry (DSC) revealed the absence of crystalline glimepiride in the S-SNEDDS. The in vitro dissolution studies revealed that the significant improvement in glimepiride release characteristics. The effect of S-SNEDDS on therapeutic efficacy of glimepride was assessed in albino rabbits by monitoring blood glucose levels and compared with free drug suspension, L-SNEDDS. The S-SNEDDS showed significant (p50.05) increase in in vitro drug release and therapeutic efficacy as compared with free drug. Conclusion: This study demonstrated that S-SNEDDS is a promising novel drug delivery system of glimepride to enhance oral delivery.

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Section: Introductionmentioning

confidence: 99%

Solid self-nanoemulsifying drug delivery system (S-SNEDDS) for oral delivery of glimepiride: development and antidiabetic activity in albino rabbits

Mohd¹,

Sanka²,

Bandi³

et al. 2014

Drug Delivery

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“…In fact, solubility enhancement is a function of surfactant concentration. This relationship generally can be found for different surfactants and different compounds (3,7,8).…”

Section: Introductionmentioning

confidence: 75%

“…Micellar drug solubilization is affected by many factors: the nature of the surfactant and the drug substance (e.g., nonpolar molecules are solubilized in the micellar core, whereas those with intermediate polarity are distributed along the surfactant molecules in certain intermediate positions), temperature, pH, and ionic strength (3,6). For ionic surfactants, the CMC values decrease and the micel-*Corresponding author.…”

Section: Introductionmentioning

confidence: 99%

Rationale for Selection of Dissolution Media: Three Case Studies

Fotaki¹,

Brown

Kochling

et al. 2013

Dissolution Technol.

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The selection of media in dissolution method development can sometimes be an arbitrary decision. The case studies in this article give a practical rationale that should help in selecting media, especially surfactants.Three cases were studied: (1) the role of surfactants versus compound stability in the dissolution medium during dissolution method development, (2) the selection of a surfactant based on interactions between the dissolution medium and the drug substance, and (3) the selection of media based on formulation properties.In the first case study, the choice of surfactant in relation to solubility and physical stability of the drug substance is shown. The second revealed an unexpected synergy between polysorbate 20 (Tween) and acetic acid solution that caused an unusual increase in the dissolution rate compared with these media used separately. In the last case study, the medium was modified by addition of surfactant to reflect a change in the formulation.The selection of a dissolution medium should be based on drug substance and formulation characteristics as well as on interactions among components.

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“…Phenylephrine, being slightly water soluble and subject to extensive presystemic metabolism in the gut wall and the liver, 6,7 was investigated as the model drug in this study. Conventional formulation approaches for water-solubility enhancement include co-grinding with surfactants, 8,9 formation of solid dispersions, 10,11 and inclusion complexes with hydrophilic cyclodextrins. [12][13][14][15] In addition to these techniques, particle size reduction to the nanometer range has also been utilized.…”

Section: Introductionmentioning

confidence: 99%

Particle size reduction to the nanometer range: a promising approach to improve buccal absorption of poorly water-soluble drugs

Rao¹,

Song²,

Peddie³

et al. 2011

IJN

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Poorly water-soluble drugs, such as phenylephrine, offer challenging problems for buccal drug delivery. In order to overcome these problems, particle size reduction (to the nanometer range) and cyclodextrin complexation were investigated for permeability enhancement. The apparent solubility in water and the buccal permeation of the original phenylephrine coarse powder, a phenylephrine–cyclodextrin complex and phenylephrine nanosuspensions were characterized. The particle size and particle surface properties of phenylephrine nanosuspensions were used to optimize the size reduction process. The optimized phenylephrine nanosuspension was then freeze dried and incorporated into a multi-layered buccal patch, consisting of a small tablet adhered to a mucoadhesive film, yielding a phenylephrine buccal product with good dosage accuracy and improved mucosal permeability. The design of the buccal patch allows for drug incorporation without the need to change the mucoadhesive component, and is potentially suited to a range of poorly water-soluble compounds.

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Surfactant-mediated dissolution: Contributions of solubility enhancement and relatively low micelle diffusivity

Cited by 127 publications

References 34 publications

Solid self-nanoemulsifying drug delivery system (S-SNEDDS) for oral delivery of glimepiride: development and antidiabetic activity in albino rabbits

Solid self-nanoemulsifying drug delivery system (S-SNEDDS) for oral delivery of glimepiride: development and antidiabetic activity in albino rabbits

Rationale for Selection of Dissolution Media: Three Case Studies

Particle size reduction to the nanometer range: a promising approach to improve buccal absorption of poorly water-soluble drugs

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