Self-Nanoemulsifying Drug Delivery System of Nifedipine: Impact of Hydrophilic–Lipophilic Balance and Molecular Structure of Mixed Surfactants
Journal Title: AAPS PharmSciTech - Year 2014, Vol 15, Issue 2
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.
Authors and Affiliations
Yotsanan Weerapol, Sontaya Limmatvapirat, Jurairat Nunthanid, Pornsak Sriamornsak
Small-Scale Assays for Studying Dissolution of Pharmaceutical Cocrystals for Oral Administration
The purpose of this study was to better understand the dissolution properties and precipitation behavior of pharmaceutical cocrystals of poorly soluble drugs for the potential for oral administration based on a small-sca...
Challenges and Strategies in Thermal Processing of Amorphous Solid Dispersions: A Review
Thermal processing of amorphous solid dispersions continues to gain interest in the pharmaceutical industry, as evident by several recently approved commercial products. Still, a number of pharmaceutical polymer carriers...
Quality-by-Design II: Application of Quantitative Risk Analysis to the Formulation of Ciprofloxacin Tablets
The online version of this article (doi:10.1208/s12249-015-0349-2) contains supplementary material, which is available to authorized users.
Efficacy, Pharmacokinetics, and Biodistribution of Thermosensitive Chitosan/β-Glycerophosphate Hydrogel Loaded with Docetaxel
Docetaxel (DTX) is a widely used anticancer drug for various solid tumors. However, its poor solubility in water and lack of specification are two limitations for clinical use. The aim of the study was to develop a therm...
Transcutaneous Peptide Immunotherapy of Japanese Cedar Pollinosis Using Solid-in-Oil Nanodispersion Technology
The online version of this article (doi:10.1208/s12249-015-0333-x) contains supplementary material, which is available to authorized users.