Formulation design and bioavailability assessment of lipidic self-emulsifying formulations of halofantrine

Khoo, Shui‐Mei; Humberstone, Andrew; Porter, Christopher John; Edwards, Glenn A.; Charman, William N.

doi:10.1016/s0378-5173(98)00054-4

Cited by 324 publications

(184 citation statements)

References 21 publications

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“…Globule Size, Zeta Potential, and Polydispersibility Index Drug release and subsequent absorption are largely influenced by the globule size of NE (23). Rapid diffusion of drug from smaller droplets into aqueous phase favors drug dissolution.…”

Section: Characterization Of Nementioning

confidence: 99%

Product Development Studies on Surface-Adsorbed Nanoemulsion of Olmesartan Medoxomil as a Capsular Dosage Form

2012

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Abstract. The present study aimed at development of capsular dosage form of surface-adsorbed nanoemulsion (NE) of olmesartan medoxomil (OLM) so as to overcome the limitations associated with handling of liquid NEs without affecting their pharmaceutical efficacy. Selection of oil, surfactant, and cosurfactant for construction of pseudoternary phase diagrams was made on the basis of solubility of drug in these excipients. Rationally selected NE formulations were evaluated for percentage transmittance, viscosity, refractive index, globule size, zeta potential, and polydispersity index (PDI). Formulation (F3) comprising of Capmul MCM® (10% v/v), Tween 80® (11.25% v/v), polyethylene glycol 400 (3.75% v/v), and double-distilled water (75% v/v) displayed highest percentage cumulative drug release (%CDR; 96.69± 1.841), least globule size (17.51±5.87 nm), low PDI (0.203±0.032), high zeta potential (−58.93±0.98 mV), and hence was selected as the optimized formulation. F3 was adsorbed over colloidal silicon dioxide (2 ml/400 mg) to produce free-flowing solid surface-adsorbed NE that presented a ready-to-fill capsule composition. Conversion of NE to surface-adsorbed NE and its reconstitution to NE did not affect the in vitro release profile of OLM as the similarity factor with respect to NE was found to be 66% and 73% respectively. The %CDR after 12 h for optimized NE, surface-adsorbed NE, and reconstituted NE was found to be 96.69±0.54, 96.07±1.76, and 94.78±1.57, respectively (p>0.05). The present study established capsulated surfaceadsorbed NE as a viable delivery system with the potential to overcome the handling limitations of NE.

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Section: Characterization Of Nementioning

confidence: 99%

Product Development Studies on Surface-Adsorbed Nanoemulsion of Olmesartan Medoxomil as a Capsular Dosage Form

2012

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“…• Dispersion time and precipitation assessment Dispersion time is defined as the time taken for lipid or surfactant based system to disperse in the dispersion medium (Khoo et al, 1998). In case of SMEDDS, it determines the time taken for pre-concentrate to form a well-dispersed, clear microemulsion.…”

Section: Evaluation Of Fl Loaded Smeddsmentioning

confidence: 99%

“…Evaluation of self-emulsifying properties of SMEDDS formulation was carried out by visual assessment as previously reported (Khoo et al, 1998). Briefly, different compositions having oil and different surfactant to co-surfactant ratios of were categorized on apparent clarity of the resultant emulsion.…”

Section: Self Emulsification and Flowabilitymentioning

confidence: 99%

Design and optimization of self-microemulsifying drug delivery system (SMEDDS) of felodipine for chronotherapeutic application

Storti-Filho

Damke

Carrara

et al. 2014

Braz. J. Pharm. Sci.

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The objective of this research work was to design, develop and optimize the self micro-emulsifying drug delivery system (SMEDDS) of Felodipine (FL) filled in hard gelatine capsule coated with polymer in order to achieve rapid drug release after a desired time lag in the management of hypertension. Microemulsion is composed of a FL, Lauroglycol FCC, Transcutol P and Cremophor EL. The optimum surfactant to co-surfactant ratio was found to be 2:1. The resultant microemulsions have a particle size in the range of 65-85 nm and zeta potential value of -13.71 mV. FL release was adequately adjusted by using pH independent polymer i.e. ethyl cellulose along with dibutyl phthalate as plasticizer. Influence of formulation variables like viscosity of polymer, type of plasticizer and percent coating weight gain was investigated to characterize the time lag. The developed formulation of FL SMEDDS capsules coated with ethyl cellulose showed time lag of 5-7 h which is desirable for chronotherapeutic application.Uniterms: Felodipine/self-microemulsifying delivery. Felodipine/chronotherapeutic application. Selfmicroemulsifying drug delivery system/development. Drugs/controlled release. Ethyl cellulose/drugs coated. Hypertension/treatment. Chronotherapeutics/hypertension treatment.O objetivo desse trabalho de pesquisa foi planejar, desenvolver e otimizar sistema de liberação de fármaco auto-microemulsificante(SMEDDS) de felodipino (FL) em cápsulas de gelatina dura revestidas com polímero, a fim de obter liberação rápida após tempo desejado no manejo da hipertensão. A microemulsão é composta de FL, lauroglilcol FCC, Transcutol P e Cremophor EL. A proporção ótima de tensoativo e de co-tensoativo foi de 2:1. As microemulsões resultantes têm tamanho de partícula na faixa de 65-85 nm com potencial zeta de -13,71 mV. A liberação de FL foi ajustada adequadamente, utilizando-se polímero independente de pH, como etilcelulose com ftalato de dibutila como plastificante. A influência das variáveis da formulação, como viscosidade do polímero, tipo de plastificante e ganho percentual de peso do revestimento foi investigada para caracterizar o intervalo de tempo de liberação. A formulação de cápsulas de FL SMEDDS revestidas com etilcelulose mostrou intervalo de tempo de liberação de 5 a 7 horas, o que é desejável para uma aplicação cronoterapêutica.Uniterms: Felodipino/liberação de fármaco auto-emulsificante. Felodipino/aplicação cronoterapêutica. Sistema de liberação de fármaco auto-emulsificante/desenvolvimento. Fármacos/liberação controlada. Etilcelulose/revestimento de fármacos. Hipertensão/tratamento. Cronoterapia/tratamento da hipertensão.

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“…Moreover, SEDDS is easy to formulate and can be easily administered in the form of soft gelatin or hard gelatin capsules. SEDDS has become favorite formulation strategy for poorly water-soluble and poorly bioavailable drugs not only in research fraternity [11][12][13][14][15][16][17][18][19][20][21] but is also accepted by pharmaceutical industries at large. To name a few, Sandimmune ® and Sandimmune Neoral There has been extensive research on the materials used for preparing SEDDS.…”

Section: Original Articlementioning

confidence: 99%

Untitled

Butani

2016

AJP

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Aims: The aim of this study was to formulate a self-microemulsifying drug delivery system (SMEDDS) of Lercanidipine HCl (LCH) using medium chain (MC) and short chain (SC) glycerides as oil phase and to compare the dissolution efficiency of both formulations. Materials and Methods: Different oils and surfactants containing MC and SC fatty acid as basic molecule were screened using quantitative solubility study and constructing pseudoternary phase diagrams. Cosolvents were used as cosurfactants. The preconcentrates were tested for a self-microemulsifying time, % transmittance, cloud point, globule size, zeta potential, and in-vitro drug release. Selected formulations were compared by calculating dissolution efficiencies in different pH media. Results: Capmul MCM, Cremophor ® RH 40, and polyethylene glycol 400 were chosen as oil, surfactant, and cosurfactant, respectively, for MC glyceride and triacetin and Tween 80 were selected as oil and surfactant for SC triglyceride category, respectively. All the formulations spontaneously resulted into transparent microemulsion with globule sizes range from 50 to 90 nm for MC-SMEDDS and 200-317 nm for SC-SMEDDS. The formed microemulsions were stable as shown by zeta potential and cloud point determination. However, in-vitro drug release in 0.1 N HCl showed quite a similar dissolution of all the formulation batches, a study in the different pH media showed that LCH being weak base, possess pH dependent solubility. Conclusions: The MC-SMEDDS were able to resist the effect of pH on dissolution to some extent as compared to pure untreated LCH and simple mixture of oil and surfactant. This piece of research strongly established the need for biorelevant dissolution interphase to differentiate between the formulations.

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Formulation design and bioavailability assessment of lipidic self-emulsifying formulations of halofantrine

Cited by 324 publications

References 21 publications

Product Development Studies on Surface-Adsorbed Nanoemulsion of Olmesartan Medoxomil as a Capsular Dosage Form

Product Development Studies on Surface-Adsorbed Nanoemulsion of Olmesartan Medoxomil as a Capsular Dosage Form

Design and optimization of self-microemulsifying drug delivery system (SMEDDS) of felodipine for chronotherapeutic application

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