Background/Objectives: This study aimed to fabricate, optimize, and characterize nanostructured lipid carriers (NLCs) loaded with trans-resveratrol (TRES) as an anti-cancer drug for pulmonary drug delivery using medical nebulizers. Methods: Novel TRES-NLC formulations (F1–F24) were prepared via hot, high-pressure homogenization. One solid lipid (Dynasan 116) was combined with four liquid lipids (Capryol 90, Lauroglycol 90, Miglyol 810, and Tributyrin) in three different ratios (10:90, 50:50, and 90:10 w/w), with a surfactant (Tween 80) in two different concentrations (0.5 and 1.5%), and a co-surfactant, soya phosphatidylcholine (SPC S-75; 50 mg). Results: Amongst the analyzed 24 TR-NLC formulations, F8, F14, and F22 were selected based on their physicochemical stability when freshly prepared and following storage (4 weeks 25 °C), as well as in terms of particle size (<145 nm), polydispersity index (PDI; 96%). Furthermore, F14 showed greater stability at 4 and 25 °C for six months and exhibited enhanced aerosolization performance, demonstrating the greater deposition of TRES in the later stages of the next-generation impactor (NGI) when using an air-jet nebulizer than when using an ultrasonic nebulizer. The F14 formulation exhibited greater stability and release in acetate buffer (pH 5.4), with a cumulative release of 95%. Conclusions: Overall, formulation F14 in combination with an air-jet nebulizer was identified as a superior combination, demonstrating higher emitted dose (ED; 80%), fine particle dose (FPD; 1150 µg), fine particle fraction (FPF; 24%), and respirable fraction (RF; 94%). These findings are promising in the optimization and development of NLC formulations, highlighting their versatility and targeting the pulmonary system via nebulization.

Background and objective: Dry powder inhalation provide many promising features for drug delivery to the pulmonary system, such as localization of drug within the lungs, drug retention in the respiratory tract, and reduced systemic toxicities. This study aimed to prepare dry powders of liposomes containing salbutamol sulfate using spray drying and study the influence of carrier type and concentration on liposome size and drug entrapment following rehydration of liposomal powder. Methods: Ethanol based proliposomes technique was used to generate liposomes containing salbutamol sulfate. Carbohydrate carriers: lactose, trehalose, sucrose, and mannitol in 1:6 or 1:10 (w/w) lipid to carrier ratio were separately incorporated into liposome formulations and dried by Büchi Mini-SprayDryerB-290. The protective effects of the sugars were investigated in terms of product yield (%), volume median diameter and size distribution of liposomes and entrapment efficiency of the drug. Results: The product yield (%) of spray dried liposome formulations with carriers was in the following order; trehalose (94.02 ± 1.20%) > sucrose (69.91 ± 1.75%) > lactose (68.30 ± 1.14%) > mannitol (50.16±0.80%) for the 1:6 formulations. Depending on the carrier type and lipidto carrier ratio, the vesicle size of liposomes with lactose and mannitol increased significantly (P 0.05) compared to the control formulations (3.6µm ±0.24). For 1:10formulation, the vesicle size with mannitol (P <0.001) and sucrose (P <0.001) increased significantly. The drug entrapment efficiency using the 1:6 formulations was 20.74±1.78% for sucrose, 35.59±2.42% for trehalose, 67.21±1.89 % for lactose, and 80.84±3.64% for mannitol. Conclusion: Stable spray-dried liposomes were manufactured using sugars as carriers. The findings of this study have demonstrated the potential using of carbohydrate carriers to increase the physical stability of liposomes during the drying process, and trehalose can offer formulations with most desirable characteristics, while mannitol showed the least benefits.

The buccal delivery is an attractive route to improve the clinical efficacy of ropinirole hydrochloride (RH) for the treatment of Parkinson and restless syndrome since this drug undergoes extensive first-pass effect, which has only 50% bioavailability after oral administration. The purpose of this study was to develop and optimize the formulation of fast disintegrating buccal effervescent tablets of RH using four types of superdisintegrants. The direct compression method was used to develop four different formulas containing RH using Kyron T-314, crospovidone, croscarmellose sodium, and sodium starch glycolate separately as a superdisintegrant. Sodium bicarbonate and citric acid were added to the formulations to produce effervescence, while sodium carbonate was used as a pH adjusting agent. All the prepared formulas were evaluated, in terms of weight variation, friability, content dose uniformity, hardness, disintegration, and dissolution test. The best formulation was selected for the subsequent study. The obtained results from pre-compression studies were in acceptable range according to British Pharmacopoeia. All formulas passed through the quality control test and significant difference (P < 0.05) was observed for the formula four compared to other formulas, due to the presence of Kyron T-314 as a superdisintegrant in formulation number 4. RH cloud be prepared as a buccal effervescent tablet and superdisintegrant provide fast disintegration of the tablet to exert rapid action.

Background and objective: Poorly water-soluble dugs provide less dissolution rate and bioavailability; hence, it minimizes the pharmacological effect of orally administered medications. Gliclazide is a sulfonylurea antidiabetic medication of the second generation, used to treat type II diabetes mellitus. It belongs to the class II drugs of biopharmaceutic classification system, indicating that it has high permeability and poor aqueous solubility. The aim of this study is to determine an optimum solid dispersion method and drug to carrier ratio to improve the solubility of gliclazide. Methods: Solid dispersions of gliclazide were formulated with polyvinyl pyrrolidone K30 using various drug to carrier ratios (1:1, 1:3, and 1:5) by utilizing kneading and solvent evaporation methods. Solubility and dissolution rate of solid dispersion formulas were compared with pure drug and co-ground mixtures. The formulations were further evaluated in terms of percentage of yield, drug content, FTIR, SEM, DSC, and XRD studies. Results: The highest solubility improvement of gliclazide was obtained at the ratio 1:5 of gliclazide and PVP K30 utilizing solvent evaporation method, solubility increased about 2.54 folds (98.299 ± 5.77 µg/ml) as compared to pure gliclazide (38.739 µg/ml). Meanwhile, the greatest improvement in gliclazide dissolution rate was observed in the same solid dispersion formula that was about 105.76 % after 30 minutes. FTIR demonstrated no unwanted interaction between the drug and carrier. While, SEM, DSC, and XRD showed crystallinity of the drug was minimized and converted to amorphous form in solid dispersion formula. Conclusion: Based on the investigations of this study, it can be concluded that the drug to carrier weight ratios and preparation methods had the influence on the drug solubility and the release rate. The obtained data revealed that the solvent evaporation is the best method of solid dispersion for enhancing gliclazide solubility using PVP K30 with the ratio 1:5 of the drug and carrier.