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. 2014 Apr;15(2):456-64.
doi: 10.1208/s12249-014-0078-y. Epub 2014 Jan 23.

Self-nanoemulsifying drug delivery system of nifedipine: impact of hydrophilic-lipophilic balance and molecular structure of mixed surfactants

Yotsanan Weerapol  1 , Sontaya Limmatvapirat, Jurairat Nunthanid, Pornsak Sriamornsak
Affiliations

Self-nanoemulsifying drug delivery system of nifedipine: impact of hydrophilic-lipophilic balance and molecular structure of mixed surfactants

Yotsanan Weerapol et al. AAPS PharmSciTech. 2014 Apr.

Abstract

A simple but novel mixed surfactant system was designed to fabricate a self-nanoemulsifying drug delivery system (SNEDDS) based on hydrophilic-lipophilic balance (HLB) value. The impacts of HLB and molecular structure of surfactants on the formation of SNEDDS were investigated. After screening various oils and surfactants, nifedipine (NDP)-loaded liquid SNEDDS was formulated with Imwitor(®) 742 as oil and Tween(®)/Span(®) or Cremophor(®)/Span(®) as mixed surfactant. Droplet size of the emulsions obtained after dispersing SNEDDS containing Tween(®)/Span(®) in aqueous medium was independent of the HLB of a mixed surfactant. The use of the Cremophor(®)/Span(®) blend gave nanosized emulsion at higher HLB. The structure of the surfactant was found to influence the emulsion droplet size. Solid SNEDDS was then prepared by adsorbing NDP-loaded liquid SNEDDS comprising Cremophor(®) RH40/Span(®) 80 onto Aerosil(®) 200 or Aerosil(®) R972 as inert solid carrier. Solid SNEDDS formulations using higher amounts (30-50% w/w) of Aerosil(®) 200 exhibited good flow properties with smooth surface and preserved the self-emulsifying properties of liquid SNEDDS. Differential scanning calorimetry and X-ray diffraction studies of solid SNEDDS revealed the transformation of the crystalline structure of NDP due to its molecular dispersion state. In vitro dissolution study demonstrated higher dissolution of NDP from solid SNEDDS compared with NDP powder.

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Figures

Fig. 1
Fig. 1
Chemical structure of the surfactants investigated in this study
Fig. 2
Fig. 2
a, b Droplet size of emulsions containing Imwitor® 742 and Cremophor®/Span® system (ratio of 1:1) as a function of HLB. Diamond Cremophor® RH40/Span® 20, square Cremophor® RH40/Span® 80, triangle Cremophor® EL/Span® 20, and circle Cremophor® EL/Span® 80
Fig. 3
Fig. 3
a, b Droplet size of emulsions containing Imwitor® 742 and Tween®/Span® system (ratio of 1:1) as a function of HLB. Diamond Tween® 80/Span® 20, square Tween® 80/Span® 80, triangle Tween® 20/Span® 20, and circle Tween® 20/Span® 80
Fig. 4
Fig. 4
Schematic representation of the micellar configuration into oil-in-water (nano)emulsion containing a Cremophor®/Span® 80, b Cremophor®/Span® 20, and c Tween®/Span®80
Fig. 5
Fig. 5
SEM images of a Aerosil® 200, b Aerosil® R972, c solid SNEDDS containing 40% Aerosil® 200, and d solid SNEDDS containing 40% Aerosil® R972
Fig. 6
Fig. 6
DSC thermograms of NDP, physical mixture, SNEDDS, and solid SNEDDS formulations containing Cremophor® RH40 and Span® 80. NDP nifedipine, A Aerosil® 200, R Aerosil® R972, PMA physical mixture of NDP and Aerosil® 200, PMR physical mixture of NDP and Aerosil® R972, A20 solid SNEDDS containing 20% Aerosil® 200, A50 solid SNEDDS containing 50% Aerosil® 200, R20 solid SNEDDS containing 20% Aerosil® R972, R50 solid SNEDDS containing 50% Aerosil® R972
Fig. 7
Fig. 7
Powder X-ray diffractograms of NDP, physical mixture, SNEDDS, and solid SNEDDS formulations containing Cremophor® RH40 and Span® 80. NDP nifedipine, A Aerosil® 200, R Aerosil® R972, PMA physical mixture of NDP and Aerosil® 200, PMR physical mixture of NDP and Aerosil® R972, A20 solid SNEDDS containing 20% Aerosil® 200, A50 solid SNEDDS containing 50% Aerosil® 200, R20 solid SNEDDS containing 20% Aerosil® R972, R50 solid SNEDDS containing 50% Aerosil® R972
Fig. 8
Fig. 8
Percentage of NDP released from different formulations, in SGF, at 37°C. Diamond liquid SNEDDS filled in hard capsule, square A50, triangle A40, and circle NDP powder. NDP nifedipine, A50 solid SNEDDS containing 50% Aerosil® 200, A40 solid SNEDDS containing 40% Aerosil® 200
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