Development and oral bioavailability assessment of a supersaturated self-microemulsifying drug delivery system (SMEDDS) of albendazole

Mukherjee, Tusharmouli; Plakogiannis, Fotios M.

doi:10.1111/j.2042-7158.2010.01149.x

Cited by 55 publications

(40 citation statements)

References 31 publications

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“…The solubility increase upon acidification complies with the fact that CN is a weak base and its solubility increases with decreasing pH (Gu et al, 2005). Similar results have been obtained with other weakly basic drugs, such as albendazole, which was shown to present increased solubility with increased concentrations of acidified PEG 400 in the formulation (Mukherjee, Plakogiannis, 2010). The solubility increase upon formulation FIGURE 1 -Influence of external formulation acidification on CN solubility.…”

Section: Influence Of External Acidification On Cn Solubilitysupporting

confidence: 69%

“…The base design suggested U_Pseudo coding with 16 runs for the fitting of a quadratic model, a check for lack of fit, and an estimate of experimental error (Mukherjee, Plakogiannis, 2010).…”

Section: Ol/i308/cr-el Systemmentioning

confidence: 99%

“…Data transformation was performed if necessary. Model fitting was carried out to select a model with insignificant lackof-fit, high adjusted and predicted R-squared values, small standard deviation, small predicted residual sum of squares (press), and no aliasing (Mukherjee, Plakogiannis, 2010).…”

Section: Experimentally Designed Phase Diagramsmentioning

confidence: 99%

“…In the current study, all phase diagrams were constructed using advanced experimental design in order to reduce the number of experiments, save time, and obtain a comprehensive analysis of the data. Design Expert® (version 9, Stat-Ease, Inc., USA) was used to construct the D-optimal mixture design (Mukherjee, Plakogiannis, 2010) of CN-SNEFs. The mixture study included three components: the oil portion (represented by free fatty acid, A), the co-surfactant portion (represented by I308, B), and the surfactant portion (represented by Cr-El, C).…”

Section: Experimentally Designed Phase Diagramsmentioning

confidence: 99%

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Optimization of self-nanoemulsifying formulations for weakly basic lipophilic drugs: role of acidification and experimental design

Shahba

Kazi

Alanazi

et al. 2016

Braz. J. Pharm. Sci.

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Formulators face great challenges in adopting systematic approaches for designing self-nanoemulsifying formulations (SNEFs) for different drug categories. In this study, we aimed to build-up an advanced SNEF development framework for weakly basic lipophilic drugs, such as cinnarizine (CN). First, the influence of formulation acidification on CN solubility was investigated. Second, formulation self-emulsification in media with different pH was assessed. Experimentally designed phase diagrams were also utilized for advanced optimization of CN-SNEF. Finally, the optimized formulation was examined using cross polarizing light microscopy for the presence of liquid crystals. CN solubility was significantly enhanced upon external and internal acidification. Among the various fatty acids, oleic acid-based formulations showed superior self-emulsification in all the tested media. Surprisingly, formulation turbidity and droplet size significantly decreased upon equilibration with CN. The design was validated using oleic acid/ Imwitor308/Cremophor El (25/25/50), which showed excellent self-nanoemulsification, 43-nm droplet size (for CN-equilibrated formulations), and 88 mg/g CN solubility. In contrast to CN-free formulations, CN-loaded SNEF presented lamellar liquid crystals upon 50% aqueous dilution. These findings confirmed that CN-SNEF efficiency was greatly enhanced upon drug incorporation. The adopted strategy offers fast and accurate development of SNEFs and could be extrapolated for other weakly basic lipophilic drugs. Uniterms: Self-nanoemulsifying formulations/solubility. Cinnarizine/lipophilic drugs. Acidification/ experimental design. Solubility enhancement.

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Section: Influence Of External Acidification On Cn Solubilitysupporting

confidence: 69%

Section: Ol/i308/cr-el Systemmentioning

confidence: 99%

Section: Experimentally Designed Phase Diagramsmentioning

confidence: 99%

Section: Experimentally Designed Phase Diagramsmentioning

confidence: 99%

See 2 more Smart Citations

Optimization of self-nanoemulsifying formulations for weakly basic lipophilic drugs: role of acidification and experimental design

Shahba

Kazi

Alanazi

et al. 2016

Braz. J. Pharm. Sci.

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“…Recently, a formulation with a high ABZ concentration was prepared by complexation with hydroxypropyl-b-cyclodextrin (25,26). Lately, a lipid based delivery system of ABZ, the self-microemulsifying drug delivery system (SMEDDS) for improving ABZ solubility, was published (27).…”

mentioning

confidence: 99%

Formulation development of an albendazole self-emulsifying drug delivery system (SEDDS) with enhanced systemic exposure / Razvoj samoemulzifirajućeg sustava za isporuku albendazola (SEDDS) s pojačanom sistemskom apsorpcijom

Meena¹,

Sharma

Kandaswamy

et al. 2012

Acta Pharmaceutica

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Most of the new chemical entities (NCEs) are poorly water-soluble and pose a challenge to developing an optimum solid oral dosage form. Oral route has been the major route of drug delivery for the treatment of various diseases. Delivery of poorly water--soluble molecules by oral route is difficult because approximately 40 % of drug compounds are limited to low aqueous solubility, which leads to restricted oral bioavailability, high intra-and inter-subject variability and lack of dose proportionality (1).To increase the oral bioavailability of poorly water-soluble compounds and eliminate the discussed drawbacks, various other formulation strategies have been adopted, including the use of cyclodextrins, nanoparticles, solid dispersions and permeation en- The aim of the study was to develop and evaluate a self--emulsifying drug delivery system (SEDDS) formulation to improve solubility and dissolution and to enhance systemic exposure of a BCS class II anthelmetic drug, albendazole (ABZ). In the present study, solubility of ABZ was determined in various oils, surfactants and co-surfactants to identify the microemulsion components. Pseudoternary phase diagrams were plotted to identify the microemulsification existence area. SEDDS formulation of ABZ was prepared using oil (Labrafac Lipopfile WL1349) and a surfactant/co-surfactant (Tween 80/PEG 400) mixture and was characterized by appropriate studies, viz., microemulsifying properties, droplet size measurement, in vitro dissolution, etc. Finally, PK of the ABZ SEDDS formulation was performed on rats in parallel with suspension formulation. It was concluded that the SEDDS formulation approach can be used to improve the dissolution and systemic exposure of poorly water-soluble drugs such as ABZ.

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Assembly of nanostructured lipid carriers loaded gefitinib and simvastatin as hybrid therapy for metastatic breast cancer: Codelivery and repurposing approach

Sherif

Shahba

Nasr

et al. 2023

Drug Development Research

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Breast cancer represents a life‐threatening problem globally. The major challenge in the clinical setting is the management of cancer resistance and metastasis. Hybrid therapy can affect several cellular targets involved in carcinogenesis with a lessening of adverse effects. Therefore, the current study aims to assemble, and optimize a hybrid of gefitinib (GFT) and simvastatin (SIM)‐loaded nanostructured lipid carrier (GFT/SIM‐NLC) to combat metastatic and drug‐resistant breast cancer. GFT/SIM‐NLC cargos were prepared using design of experiments to investigate the impact of poloxamer‐188 and fatty acids concentrations on the physicochemical and pharmaceutical behavior properties of NLC. Additionally, the biosafety of the prepared GFT/SIM‐NLC was studied using a fresh blood sample. Afterward, the optimized formulation was subjected to an MTT assay to study the cytotoxic activity of GFT/SIM‐NLC compared to free GFT/SIM using an MCF‐7 cell line as a surrogate model for breast cancer. The present results revealed that the particle size of the prepared NLC ranged from (209 to 410 nm) with a negative zeta potential value ranging from (−17.2 to −23.9 mV). Moreover, the optimized GFT/SIM‐NLC formulation showed favorable physicochemical properties and promising lymphatic delivery cargos. A biosafety study indicates that the prepared NLC has a gentle effect on erythrocyte hemolysis. Cytotoxicity studies revealed that GFT/SIM‐NLC enhanced the killing of the MCF‐7 cell line compared to free GFT/SIM. This study concluded that the hybrid therapy of GFT/SIM‐NLC is a potential approach to combat metastatic and drug‐resistant breast cancer.

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Development and oral bioavailability assessment of a supersaturated self-microemulsifying drug delivery system (SMEDDS) of albendazole

Abstract: This study demonstrates a strategy for the development of a supersaturated SMEDDS formulation of a drug with low aqueous solubility.

Cited by 55 publications

References 31 publications

Optimization of self-nanoemulsifying formulations for weakly basic lipophilic drugs: role of acidification and experimental design

Optimization of self-nanoemulsifying formulations for weakly basic lipophilic drugs: role of acidification and experimental design

Formulation development of an albendazole self-emulsifying drug delivery system (SEDDS) with enhanced systemic exposure / Razvoj samoemulzifirajućeg sustava za isporuku albendazola (SEDDS) s pojačanom sistemskom apsorpcijom

Assembly of nanostructured lipid carriers loaded gefitinib and simvastatin as hybrid therapy for metastatic breast cancer: Codelivery and repurposing approach

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