SEDDS

Various strategies have been widely investigated to enhance the solubility of poorly soluble drugs. These strategies increase the clinical efficacy when the drug is administered orally. Around 40% of novel chemical entities show evidence of poor aqueous solubility and their bioavailability becomes low. Thus to overcome this problem new technologies are applied. This new technologies improve the solubility of those drugs whose water solubility is poor. This new technology is known as SEDDS. Self-emulsifying drug delivery systems (SEDDS), which are isotropic mixtures of oils, surfactants, solvents and co-solvents/surfactants, can be used for the design of formulations in order to improve the oral absorption of highly lipophilic drug compounds. It can be orally administered in soft or hard gelatin capsules. This formulation enhanced bioavailability due to increase the solubility of drug and minimizes the gastric irritation.

The aim of present work was to develop a self emulsifying emulsion of ketaconazole for the topical delivery system which is useful in the treatment of fungal infection. Prepared SEDDS was investigated for different parameters. All the prepared SEDDS showed acceptable physical properties concerning colour, viscosity, melting point etc. The results of in -vitro drug release showed that carbopol 934 was the formula of choice as it showed better drug release & antifungal activity. The percentage cumulative drug released was determined by UV spectrophotometer. FTIR studies revealed that drug and all excipients are compatible. The data obtained from in- vitro permeation studies was treated by various conventional mathematical models (zero order, first order, Higuchi and Korsmeyer- peppa’s) to determine the release mechanism from the designed self emulsifying formulations. Selection of a suitable release model was based on the values of R2 (correlation coefficient), k (release constant) obtained from the curve fitting of release data. It was found that all the formulations follows the first order kinetics. The regression coefficients for the all formulations F1 to F4 of Higuchi plot was found to be almost linear. Key words: SEDDS, ketaconazole, antifungal drug, topical drug delivery.

Aim of present study was to develop self emulsifying drug delivery system (SEDDS) for enhancement of solubility, dissolution rate and oral bioavailability of model drug Rilpivirine. Fifteen formulations were prepared using different oils, surfactants and co-surfactants. A pseudo ternary phase diagram was constructed to identify the self-micro emulsification region. Further, the resultant formulations were investigated for clarity, phase separation, drug content, % transmittance, globule size, freeze-thaw stability and in vitro dissolution studies. On the basis of dissolution profile and other above mentioned studies, F5 was found to be the best formulation of Rilpivirine SEDDS which contains Captex 355(Oil), Kolliphor RH 40 (Surfactant) and PG (Co-surfactant). In vivo studies revealed that the oral bioavailability of Rilpivirine from SEDDS was 2.2-fold higher compared to that of pure Rilpivirine suspension in rats, suggesting a significant increase (p

Ibuprofen self-emulsified drug delivery system (IBSEDDS) has been prepared, characterized and optimized to release 100% drug in one hour. The optimal formulation was subjected to stability and bioavailability studies in human volunteers. The stability was conducted under different storage temperature (4oC, room temperature and 37oC) for 8 months and evaluated for in-vitro drug release, particle size and turbidity. Bioavailability was evaluated after administration of a single oral dose of two formulations, test (HPMC capsule containing IBSEDD) and reference (HPMC capsule containing 50 mg drug in soybean oil), by 6 health human volunteers. The results showed that IBSEDDS was stable under different storage temperatures and the drug was more stable at 4oC. The changes in particle size and turbidity were lesser at room temperature.  The pharmacokinetic parameters for test/reference were: the Cmax , 0.892/0.468 ug/ml,  the Tmax, 1/1.5hr and the AUC0-∞, 3.956/1.986 mg.hr/ml. The % RBof IBSEDDS was 199.114. In a conclusion, the IBSEDD formulation stored at 4oC were more stable regarding drug content but samples stored at room temperature were more stable regarding particle size and turbidity. The IBSEDD formulation showed higher rate and extent of drug absorption and higher bioavailability compared to the oily drug solution.