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Development of self-nanoemulsifying drug delivery systems (SNEDDS) of docosahexaenoic acid (DHA) is reported with the aim to achieve enhanced dissolution rate. The optimized composition of liquid SNEDDS (L-SNEDDS) formulation was Labrafil M1944 CS, 47% v/v Tween 80, 27% v/v Transcutol P, and 0.1% v/v DHA. L-SNEDDS were solidified using Syloid XDP 3150 as solid porous carrier. The droplet size, polydispersity index, zeta potential, percentage drug loading, and cloud point for L-SNEDDS were found to be 43.51 ± 1.36 nm, 0.186 ± 0.053, −19.20 ± 1.21 mV, 93.23 ± 1.71, and 88.60 ± 2.54 °C, respectively. Similarly, for solid SNEDDS (S-SNEDDS) the above parameters were found to be 57.32 ± 1.87 nm, 0.261 ± 0.043, −16.60 ± 2.18 mV, 91.23 ± 1.88, and 89.50 ± 1.18 °C, respectively. The formulations (L-SNEDDS, S-SNEDDS powder, and S-SNEDDS tablet) showed significant (p<.05) improvement in dissolution rate of drug in 0.1 N HCl (pH 1.2) and phosphate buffer (pH 6.8) as compared to unprocessed DHA. In both the dissolution media, the dissolution rate was found more that 85% in 90 min. Absence of drug precipitation, phase separation, and turbidity during thermodynamic stability studies indicated that the developed SNEDDS were stable. Hence, it was concluded that SNEDDS have offered sufficient stability as well as dissolution rate of DHA. [ABSTRACT FROM AUTHOR]

The aim of present study was to introduce the role of quality by design to produce curcumin crystals with enhanced dissolution rate and bioavailability. The liquid antisolvent method was used to produce crystals. The crystal growth was controlled using the Box–Behnken design. The variables used in the crystallization process included the ratio of pyrocatechol to polyethylene glycol (PEG) 1500, solvent addition rate, stirring time, and stirring speed. Combination of these variables was found to yield curcumin crystals of 2.45 ± 0.56 μm size and 0.321 polydispersity index that exhibited enhanced solubility, dissolution rate, product yield, and compressibility. The optimized curcumin crystals were characterized by Fourier-transform infrared spectrophotometer (FT-IR), nuclear magnetic resonance, differential scanning calorimetry, X-ray powder diffraction, and scanning electron microscopy. The dissolution rate and oral bioavailability of optimized curcumin crystals were found to be 2.66- and 7.08-folds higher than its unprocessed form. The optimized crystals were found stable for 6 months under accelerated temperature of 40°C and 75% relative humidity as there was no significant difference observed in the crystal size and dissolution profile. [ABSTRACT FROM AUTHOR]

An attempt has been made to prepare solid self-nanoemulsifying drug delivery system (SNEDDS) of polypeptide-k (PPK) and curcumin (CRM) using Labrafil M1944 CS as oil, Tween-80 as surfactant, Transcutol P as cosurfactant and Aerosil-200 (A-200) as porous hydrophobic carrier for improving their antidiabetic potential through oral delivery. Box–Behnken Design was used to optimize the liquid formulation based on the results of the mean droplet size, polydispersity index, percentage drug loading, and zeta potential. The formulation was adsorbed on Aerosil-200 through spray drying. The formulation showed desirable micromeritic, disintegration, and dissolution properties. About fivefold rise in the dissolution and permeation rate for drugs was observed from formulations vis a vis their unprocessed forms. The formulation was found to be stable with variation in pH, dilution, and temperature. The individual solid SNEDDS formulation of PPK and CRM and their combination were evaluated for antidiabetic potential and the results were compared with their naive forms on streptozotocin-induced diabetic rats. The results revealed better control of serum glucose level and other biochemical tests, such as liver parameters, lipid profiles, and antioxidant levels, as well as histological evaluation of pancreatic tissues in all the solid SNEDDS formulation as compared with their naive forms. [ABSTRACT FROM AUTHOR]

Development of self-nanoemulsifying drug delivery systems (SNEDDS) of glimepiride is reported with the aim to achieve its oral delivery. Lauroglycol FCC, Tween-80, and ethanol were used as oil, surfactant, and co-surfactant, respectively as independent variables. The optimized composition of SNEDDS formulation (F1) was 10% v/v Lauroglycol FCC, 45% v/v Tween 80, 45% v/v ethanol, and 0.005% w/v glimepiride. Further, the optimized liquid SNEDDS were solidified through spray drying using various hydrophilic and hydrophobic carriers. Among the various carriers, Aerosil 200 was found to provide desirable flow, compression, dissolution, and diffusion. Both, liquid and solid-SNEDDS have shown release of more than 90% within 10 min. Results of permeation studies performed on Caco-2 cell showed that optimized SNEDDS exhibited 1.54 times higher drug permeation amount and 0.57 times lower drug excretion amount than that of market tablets at 4 hours (p < .01). Further, the cytotoxicity study performed on Caco-2 cell revealed that the cell viability was lower in SNEDDS (92.22% ± 4.18%) compared with the market tablets (95.54% ± 3.22%; p > .05, i.e. 0.74). The formulation was found stable with temperature variation and freeze thaw cycles in terms of droplet size, zeta potential, drug precipitation and phase separation. Crystalline glimepiride was observed in amorphous state in solid SNEDDS when characterized through DSC, PXRD, and FT-IR studies. The study revealed successful formulation of SNEDDS for glimepiride. [ABSTRACT FROM AUTHOR]

In the present study, different solid self-nanoemulsifying drug delivery system (S-SNEDDS) was formulated by using porous hydrophilic and hydrophobic carriers to improve the dissolution rate and bioavailability of simvastatin (SIM). The prepared liquid-SNEDDS composed of Labrafil M 1944 CS/ Tween-80/ Ethanol (20% / 53.33%/26.67% v /v) with 0.1% SIM, resulted droplet size of 40.69 nm. The hydrophobic carriers used were Aerosil-200, Syloid 244FP, Syloid XDP 3150, Magnesium stearate, Micro Crystalline Cellulose PH102 and lactose and hydrophilic carriers used were Poly vinyl alcohol, Sodium carboxy methyl cellulose and hydroxypropyl-β-cyclodextrin. These S-SNEDDS were characterized through micromeritic, biopharmaceutical studies and stability studies. The spray dried S-SNEDDS prepared by using Aerosil 200 as hydrophobic carrier provided nanoemulsions with unchanged droplet size and drug release when subjected at different stress conditions such as thermodynamic stress and freeze thaw cycles. In vitro dissolution studies revealed that the L-SNEDDS and S-SNEDDS of Aerosil 200 were found to be remarkably superior over the unprocessed SIM and marketed SIM. Scanning electron microscope, Differential scanning calorimeter and Powder X-Ray Diffraction revealed crystalline SIM was present in a changed amorphous state in the SNEDDS formulations prepared with Aerosil 200 as carrier. Further, pharmacokinetic study carried out on rats revealed 0.5 h increase in time for maximal concentration (T max ), 3.75 folds increase in maximal concentration (C max ), 1.22 h increase in mean residence time, 1.54 folds increase in area under curve (AUC 0-t ), 2.10 folds increase in AUC 0-∞ and 3.28 folds increase in bioavailability confirms that the developed S-SNEDDS were superior than that of marketed formulation. Hence, it can be safely concluded that Aerosil 200 based S-SNEDDS were able to provide improvement in dissolution rate and oral bioavailability of SIM. [ABSTRACT FROM AUTHOR]

Advantage of spray drying technique over the conventional surface adsorption technique for co-formulation of solid SNEDDS (S-SNEDDS) of curcumin (CRM) and duloxetine (DXH) is discussed. Liquid SNEDDS were prepared using castor oil (20% w/w), Tween-80 (40% w/w) and Transcutol® P (40% w/w) as oil, surfactant and co-surfactants containing both CRM and DXH. S-SNEDDS were formulated by adsorption of liquid SNEDDS onto porous hydrophilic and hydrophobic carriers through spray drying and surface adsorption techniques. The percentage drug loading for CRM and DXH in optimized L-SNEDDS was 87.22 ± 1.87 and 92.32 ± 0.19%, mean droplet size, 113.14 ± 1.14 nm; polydispersity index, 0.20 ± 0.026, and zeta potential − 13.2 mV, respectively. Prepared formulation was evaluated for parameters such as, oil adsorption tendency, micromeritic characteristics, disintegration and dissolution behaviour to identify suitable carrier for conversion of L-SNEDDS into S-SNEDDS. Among the carriers used, Syloid® 244FP revealed highest oil adsorption capacity. Spray drying of L-SNEDDS using Syloid® 244FP as carrier further improved micromeritic properties with lower angle of repose (22.18 ± 0.22°), higher flow rate (4.33 ± 0.26 g/s), lower true (1.23 ± 0.22 g/cm 3 ), bulk (0.202 ± 0.05 g/cm 3 ) and tapped density (0.216 ± 0.07 g/cm 3 ). In vitro dissolution and ex-vivo permeation studies revealed non-significant (P > 0.05) drugs' release from S-SNEDDS powders/tablets viz-a-viz their L-SNEDDS formulation. SNEDDS were found to be remarkably superior over the unprocessed drugs in their dissolution and permeation studies. They were found to be stable in terms of droplet size, dissolution pattern, tablet hardness and assay when subjected to stability testing. Scanning Electron Microscopy, Differential Scanning Calorimetry and powder X-ray diffraction studies revealed that crystalline drugs were converted to their amorphous state in the SNEDDS formulations. Spray drying technique has, therefore proved to distinctly improve the micromeritics and biopharmaceutical attributes in the co-formulation of curcumin and duloxetine S-SNEDDS. [ABSTRACT FROM AUTHOR]