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Objective: Zolmitriptan is a BCS class II drug having low solubility and poor bioavailability by formulating Nanostructured lipid carriers that will sustain the release of the drug for a longer period which leads to reduced dose and frequency of dose. Method: Zolmiptriptan-loaded Nanostructured lipid carriers were fabricated by a solvent diffusion evaporation method. The formulation parameters like the selection of solid (Precirol ATO 5) and liquid lipid (Miglyol 812), solid to liquid lipid ratio (3:1), drug: solid lipid ratio (1:4), the ratio of the organic phase (Acetone: Ethanol, 1:1), the concentration of surfactant (1.5% Tween 80) and temperature (70 °C) of secondary phase were optimized. NLC dispersion was finally lyophilized and converted into a tablet. A stability study of freeze-dried NLCs tablet was performed according to ICH Q1A (R2) guidelines. Result: Optimized formulation contained Particle size 11.39 ± 0.85 nm, Zeta potential -38.30 and %EE 76.56 ± 0.12. Characterization was performed by TEM and FTIR analysis. The residual solvent test confirms the concentration of organic solvents was in the acceptable range as per ICH guidelines. In-vitro drug permeation study of NLCs shows 88.91±0.238 % drug release while pure drug suspension shows 58.9±0.578 % drug release after 12 hrs. Conclusion: Zolmitriptan-loaded NLCs show better absorption as compared to pure drug suspension which indicates prolonged release of medicament which may reduce dose or dose frequency.

Nano Structured Lipid Carriers (NLCs) are potential alternative of the tradition colloidal drug carrier. The main benefit is related to the well-known concept that lipids used in nanoparticle formulation promote drug oral absorption because they go through the same physiological mechanism as food lipid digestion. The objective of the present work is to use potential carrier NLCs for the oral delivery of poorly soluble drug Febuxostat (FEB). FEB-NLCs were formulated by High Speed Homogenization with Ultra sonication method using Capmul GMS 50 K as solid lipid and Transcutol HP as a liquid lipid. The 32 full factorial design utilized to study the effect of influence of solid lipid to liquid lipid ratio and concentration of surfactant, on the particle size and entrapment efficiency. Mean particle size and entrapment efficiency were found for all prepared formulation in the range of 196.66±2.08 nm to 368.33±2.51 nm and 74.80±0.52 % to 86.47±0.749 % respectively. Zeta potential was -15.2mv which is negative enough to give good stability. TEM study shows good spherical morphology of particle with diameter less than 200nm. In-vitro and Ex-Vivo study revel that NLCs gives biphasic release of the drug; first initial burst release and then sustained release up to 24 hour. The formulated NLCs dispersion was successfully converted in to the free flowing powder using trehalose as a cryoprotectant. In conclusion, FEB-NLCs potential carrier for the oral delivery and controlled release of drug which may reduce dosing frequency and improve patient compliance.

The aim is to develop and evaluate rizatriptan benzoate (RB) loaded nanostructured lipid carriers (NLCs) that might improve oral bioavailability. NLC was prepared using High-Speed Homogenization (HSH) coupled with the ultrasonication method. Process parameters were selected on basis of the trial-and-error method which is time for homogenization, speed of homogenization, and time for sonication. Using a Design expert, 32 Full Factorial design was prepared using solid lipid to liquid lipid ratio and concentration of surfactant as independent variables. RB-NLC was evaluated on basis of particle size, %Entrapment Efficiency (EE), Zeta potential, Transmission electron microscopy (TEM), In-Vitro permeation study, and Ex-vivo permeation study. Confocal Laser Scanning Microscopy was performed to study the uptake of RB-NLC through M-Cells, and Peyer's Patches. RB-NLC dispersion was converted into free-flowing lyophilized powder using cryoprotectant which is trehalose and in vitro permeation study was performed. Among all the batches of RB-NLC, the Optimized batch was evaluated. The optimized formulation showed a particle size of 412.8 ± 1.15nm with 0.261 PDI and − 36.6mV zeta potential. It showed 84.26 ± 1.03% EE. TEM image showed a spherical shape and smooth surface area. In-Vitro and Ex-vivo studies showed 97.21 ± 0.36%CDR up to 22 hours & 61.02 ± 1.25%CDR up to 6 hours. Lyophilized powder showed 96.37 ± 0.36%CDR up to 22 hours. Based on the data we can conclude that RB-NLC increases the permeation and it may increase its Bioavailability (BA). Lyophilized powder of RB-NLC showed a sustained release pattern and it may reduce the dosing frequency of the drug.

The main objective of the research work was to improve the solubility of Bosentan by preparing Microemulsion (ME) for pulmonary artery hypertension therapy. Capmul MCM C8 was selected as oil, Tween 20 as a surfactant and Transcutol HP as a co-surfactant. From Pseudoternary phase diagram ratio of Smix (1:1) selected. From the Microemulsion area of ternary diagram different batches were prepared, but the drug was precipitate from the formulation which can be avoid by adding precipitate inhibitor. Pluronic F 127 was utilized as precipitate inhibitor in the concentration of 1.5%. The optimized formulation ME 8 contain oil (30 %V/V), Smix (60 %V/V) and water (10 %V/V). The prepared Microemulsion evaluated for globule size 96.71±0.11 nm, % transmittance 99.45±0.54 % and >99 % drug content. TEM confirm the spherical shape of globule. The physicochemical parameter of ME 8 was performed and to enhance the stability of Microemulsion it is converted in to solid ME by using adsorbent. Aeroperl 300 was selected as an adsorbent in the drug to adsorbent ratio (1:0.5 %W/W) based on physicochemical properties. From the in-vitro drug release investigation after 7 hours %CDR of ME 8 was found to be 78.87±0.17% and solid Microemulsion (SME 3) shows 76.83±0.29%. The pure drug shows only 27.63±0.23% CDR, which indicate that ME revealed better drug release than pure drug. There was a 2.8 fold increases in solubility compare to pure drug. From the In-vivo data compared to convention formulation, there was significant change in pharmacokinetics data observed.

Febuxostat loaded microballoons (FEB-MBs) were formulated using a non-aqueous solvent evaporation method using Eudragit RS 100, HPMC K4 M as a polymer, and span 80 as a surfactant. The ratio of solvents like methanol and dichloromethane, liquid paraffin as a processing medium. The formulation was optimized by the Box-Behnken design. Optimized formulation was evaluated for particle size, entrapment efficiency, % buoyancy, Percentage yield, in-vitro release studies, and stability study. Mean particle size 80.11 ± 0.349, entrapment efficient 83.25 ± 0.526, and % buoyancy 92.41 ± 0.57 were found for optimized formulation. Scanning electron microscopy (SEM) image of formulation shows discrete particle size with smooth surface texture with a hollow space and spherical shape and particle size is less than 200 µm. The result of in-vitro study shows an improved rate of drug release for a longer period from FEB-MBs compared with pure drugs. This is due to increases in the surface area leads to increases in absorption. The stability study shows no significant change in microballoons of the optimized formulation after 30 days of storage as per ICH guidelines. This multi particulate system provides an excellent approach for sustained release of a medicament for longer, thereby reducing dose frequency.