Inclusion of telmisartan in mesocellular foam nanoparticles: drug loading and release property.
Spherical mesocellular foam (MCF) with a continuous 3-D pore system was synthesized using Pluronic 123 triblock polymer (P123) as a surfactant coupled with cetyltrimethyl ammonium bromide (CTAB) as a co-surfactant. The feasibility of the prepared MCF nanoparticles for oral drug delivery was studied. A model drug, telmisartan (TEL), was loaded onto MCF via a procedure involving a combination of adsorption equilibrium and solvent evaporation. The drug-release rate and the drug loading efficiency of spherical MCF were compared with those of fibrous SBA-15. Investigations using nitrogen adsorption, scanning electron microscopy (SEM), transmission electron microscopy (TEM), wide-angle X-ray scattering (WXRS), differential scanning calorimetry (DSC) and HPLC demonstrated the successful incorporation of TEL into the MCF host. It is found that spherical MCF has a high drug loading efficiency up to 42.9% (drug weight/total weight) and higher than that of SBA-15 with a pore diameter of 6.5 nm. It is shown that a fast release rate of TEL was obtained from MCF compared with SBA-15 and pure crystalline TEL using enzyme-free simulated gastric fluid (pH 1.2) and intestinal fluid (pH 6.8). We believe that the present study will help in the design of oral drug delivery systems for the dissolution enhancement of water-insoluble drugs.
Zhang
Yanzhuo
Y
Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, PR China.
Jiang
Tongying
T
Zhang
Qiang
Q
Wang
Siling
S
D000284:Administration, Oral; D047228:Angiotensin II Type 1 Receptor Blockers / Q000008:administration & dosage / Q000737:chemistry*; D001562:Benzimidazoles / Q000008:administration & dosage / Q000737:chemistry*; D001565:Benzoates / Q000008:administration & dosage / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D000077286:Cetrimonium; D002593:Cetrimonium Compounds / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers; D004339:Drug Compounding; D005750:Gastric Juice / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D007419:Intestinal Secretions / Q000737:chemistry; D007700:Kinetics; D008855:Microscopy, Electron, Scanning; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D011060:Poloxalene / Q000737:chemistry*; D016062:Porosity; D012542:Scattering, Radiation; D012822:Silicon Dioxide / Q000737:chemistry; D012995:Solubility; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry*; D013678:Technology, Pharmaceutical / Q000379:methods; D000077333:Telmisartan
D047228:Angiotensin II Type 1 Receptor Blockers; D001562:Benzimidazoles; D001565:Benzoates; D002593:Cetrimonium Compounds; D004337:Drug Carriers; C509969:SBA-15; D013501:Surface-Active Agents; C464484:pluronic block copolymer P123; D012822:Silicon Dioxide; D011060:Poloxalene; D000077333:Telmisartan; D000077286:Cetrimonium