Preparation And Evaluation Of Solid Lipid-based Formulations

Drugs,classified as BCS II,are good membrane permeability,poorly water-soluble and low bioavailability.Lipid-based drug delivery systems have shown a greet success on imporving the oral bioavailability of poorly water-sobuble drug.Conventionally,lipid-based formulations were prepared by liquid components which had some disadvanteges as follows:complexied producation process,low drug loading and the leakage of drug during long-term storage and so on.In order to overcome the shortcome of lipid-based formulaitons,researches oin solid lipid-based drug delivery systems have developed.Solid lipid-base for mulations have combined the advantages of lipid-based systems and solid dosag e forms.Preparation of solid lipid-based formulaitons was used drying technique s including physical adsorption,spray drying,melt granulation,melt extrusion sp heronization and lyophilisation to absorb liquid formulaitons onto solid carriers.Solid lipid formulations could enhance the long-term stability of drugs and exp and the scope of application.Furthermore,the eligible solid carriers which were used to prepared solid lipid dosages could improve the solubilisation of poorly water-soluble drug in gasintestenal environment,that was favor to drug absorpti on.In this paper,CoenzymeQ10(CoQ10)was chosed as model drug to prepare the liquid lipid-based formulations.The mean size of CoQ10-loaded self-mi coemulsifying drug delivery systems(SMEDDS)and emulsion was 61.0±2.4 nm and 224.0± 1.9 nm,respectively.PDI was 0.23 ± 0.03 and 0.18 ± 0.02,respectively.Solid self-emulsifying drug delivery systems was developed by different dyring technology with magnesium aluminum silicate as solid carriers.In addition,silica lipid hybrid(SLH)microparticles was prepared via various dyring technology with silica nanoparticles as solid carriers.The redispersed mean size,surface morphology and phsicochemical characterization was studied.Surface morphology of solid SMEDDS and SLH using SEM image showed that the surface of samples was composed of the agglomerates of finely individual particles.The results of DSC and XRD were verified that entrapped CoQ10 was amorphous or molecular state in solid SMEDDS and SLH formulations In vitro dissolusion study,solid SMEDDS and SLH could improve the rate and extent of CoQ10 solubility in comparison with the pure drug powder.In present work,the drug solubilisation capability of solid formulations was evaluated under simulated fasted/fed digesting conditions using an in vitro lipolysis model,and pure coenzymeQlO powder was used as a control.Solid SMEDDS and SLH significantly enhanced the extent of drug solubilisation under fasting conditions between 10.6 and 14.8-folds,respectively,in comparison to pure drug.During a 30-day stability study,solid formulations showed terrific stability and high retention rate(above 84.42%)after stored in different temperature.All the studies demonstrated that solid lipid-based formulations could be identified as an appropriate strategy to improve solubilisation capability and stability of coenzymeQ10.