Microparticles-entrapped micelles: a novel delivery system to improve solubility and dissolution rate of poorly water-soluble valsartan

Abstract

Surfactants are routinely included in tablets during wet or dry granulations or along with directly compressible vehicles to improve wetting, disintegration and dissolution. Besides this micellar solubilization can improve permeability of poorly soluble drugs via gastrointestinal tract membranes thereby enhancing oral bioavailability. Microparticle-entrapped micelles (MEM) technology is a novel method of incorporating surfactants in tablets for improving in vitro and in vivo performance of poorly water-soluble drugs. Valsartan (VAL) was solubilized in cremophor EL micelles at cloud point temperature; lactose was dissolved in micellar dispersion and the dispersion was directly spray-dried to obtain solid product, which was subsequently converted into tablets using suitable excipients. VAL tablets produced by applying MEM technology improved dissolution performance of valsartan tablets. These tablets exhibited superior dissolution rate over controls and marketed tablets in all media employed irrespective of pH conditions and composition.

Inhibition of Bacterial Pathogens in Medium and on Spinach Leaf Surfaces using Plant‐Derived Antimicrobials Loaded in Surfactant Micelles

“…The driving force behind micelle formation is the hydrophobic effect, which causes the surfactant molecules to minimize unfavorable contact between the hydrophobic groups and the surrounding aqueous phase (McClements and others ). Surfactant micelles have been reported to increase the solubility of hydrophobic compounds, including plant essential oils (EOs) and EOCs, in aqueous systems (McClements ; Torchilin ; Parvataneni and others ). Pérez‐Conesa and others () reported that Surfynol® 485W micelles containing carvacrol and eugenol inactivated biofilms of 2 strains of E. coli O157:H7 on stainless steel.…”

Enhanced dissolution and stability of artemisinin by nano-confinement in ordered mesoporous SBA-15 particles

“…Encapsulation of drug molecules inside mesoporous carriers in amorphous form is an excellent approach to enhance the solubility of water-insoluble drugs with adequate storage stability (Rengarajan et al, 2008), compared with other solubility enhancement techniques, such as micellisation (Parvataneni et al, 2013), cyclodextrin complex (Ali et al, 2013), nanoemulsions (Liu et al, 2014), co-crystallisation (Shiraki et al, 2008), solid dispersion (Van Den Mooter, 2012) and micronisation (Rao et al, 2011). Approximately, 2643 papers related to mesoporous and drug delivery have been published in the Web of Science by 2013, which illustrates the importance of the mesoporous materials in medical applications (Xu et al, 2013).…”

Improved Dissolution and Oral Bioavailability of Valsartan Using a Solidified Supersaturable Self-Microemulsifying Drug Delivery System Containing Gelucire® 44/14

“…VST belongs to class II of the biopharmaceutical classification system (BCS) and has a low oral bioavailability (BA) because of its limited solubility in water and acidic pH environments [2]. To solve this problem, various techniques including cyclodextrin complexation, solid dispersion, microemulsification, micelles, and nanosuspension have been widely introduced [3,4,5,6]. Among these, an approach using a self-microemulsifying drug delivery system (SMEDDS) composed of oil, surfactant, and cosurfactant has been extensively investigated [7,8].…”