Ahmad Fuad Shamsuddin

Formulation optimization of palm kernel oil esters nanoemulsion-loaded with chloramphenicol suitable for meningitis treatment

Palm kernel oil esters nanoemulsion-loaded with chloramphenicol was optimized using response surface methodology (RSM), a multivariate statistical technique. Effect of independent variables (oil amount, lecithin amount and glycerol amount) toward response variables (particle size, polydispersity index, zeta potential and osmolality) were studied using central composite design (CCD). RSM analysis showed that the experimental data could be fitted into a second-order polynomial model. Chloramphenicol-loaded nanoemulsion was formulated by using high pressure homogenizer. The optimized chloramphenicol-loaded nanoemulsion response values for particle size, PDI, zeta potential and osmolality were 95.33nm, 0.238, -36.91mV, and 200mOsm/kg, respectively. The actual values of the formulated nanoemulsion were in good agreement with the predicted values obtained from RSM. The results showed that the optimized compositions have the potential to be used as a parenteral emulsion to cross blood-brain barrier (BBB) for meningitis treatment.

Formulation Optimization of a Palm-Based Nanoemulsion System Containing Levodopa

Response surface methodology (RSM) was utilized to investigate the influence of the main emulsion composition; mixture of palm and medium-chain triglyceride (MCT) oil (6%–12% w/w), lecithin (1%–3% w/w), and Cremophor EL (0.5%–1.5% w/w) as well as the preparation method; addition rate (2–20 mL/min), on the physicochemical properties of palm-based nanoemulsions. The response variables were the three main emulsion properties; particle size, zeta potential and polydispersity index. Optimization of the four independent variables was carried out to obtain an optimum level palm-based nanoemulsion with desirable characteristics. The response surface analysis showed that the variation in the three responses could be depicted as a quadratic function of the main composition of the emulsion and the preparation method. The experimental data could be fitted sufficiently well into a second-order polynomial model. The optimized formulation was stable for six months at 4 °C.

Effects of intravenous palm oil-based lipid nanoemulsion on fat metabolism in rabbits

Abstract Objective To investigate the effects of a newly-developed nanoemulsion of palm oil in combination with medium chain triglyceride (MCT) oil (NEMS®MCT/LCT20%) on fat metabolism in male New Zealand white rabbits. Methods Six rabbits were divided into two groups of three rabbits in each group. NEMS®MCT/LCT20%, Lipofundin®MCT/LCT 20% (a commercially-available lipid emulsion) and normal saline (control) were administered intravenously in these rabbits via the marginal ear vein for 6 h. Cross-over method was used in these rabbits with a wash-out period of two weeks in-between infusions. Triglyceride (TG), total cholesterol, low density lipoprotein and high density lipoprotein cholesterols were determined using enzymatic strip test at 0, 2, 4 and 6 h of infusion. Blood levels of free fatty acid (FFA) were measured at 0 and 6 h. Results Serum TG levels increased in these rabbits after 2 and 4 h infusion of NEMS®MCT/LCT20% but returned to normal after 6 h. Concentration of FFA increased in a dose-related manner but remained within the normal range (315-535 μmol/L). Similar results were obtained with Lipofundin®MCT/LCT20%. All parameters of fat metabolism in these rabbits remained unchanged from baseline when normal saline was administered. Changes in the parameters of fat metabolism measured between NEMS®MCT/LCT20% and Lipofundin®MCT/LCT20% did not show any significant difference. Significant difference ( P Conclusions Intravenous administration of NEMS®MCT/LCT20% did not cause a permanent increase in the TG level of rabbits while FFA remained within the normal range.

Development of nanoemulsion for efficient brain parenteral delivery of cefuroxime: designs, characterizations, and pharmacokinetics

Background and aim Drugs that are effective against diseases in the central nervous system and reach the brain via blood must pass through the blood–brain barrier (BBB), a unique interface that protects against potential harmful molecules. This presents a major challenge in neuro-drug delivery. This study attempts to fabricate the cefuroxime-loaded nanoemulsion (CLN) to increase drug penetration into the brain when parenterally administered. Methods The nanoemulsions were formulated using a high-pressure homogenization technique and were characterized for their physicochemical properties. Results The characterizations revealed a particle size of 100.32±0.75 nm, polydispersity index of 0.18±0.01, zeta potential of −46.9±1.39 mV, viscosity of 1.24±0.34 cps, and osmolality of 285.33±0.58 mOsm/kg, indicating that the nanoemulsion has compatibility for parenteral application. CLN was physicochemically stable within 6 months of storage at 4°C, and the transmission electron microscopy revealed that the CLN droplets were almost spherical in shape. The in vitro release of CLN profile followed a sustained release pattern. The pharmacokinetic profile of CLN showed a significantly higher Cmax, area under the curve (AUC)0–t, prolonged half-life, and lower total plasma clearance, indicating that the systemic concentration of cefuroxime was higher in CLN-treated rats as compared to cefuroxime-free treated rats. A similar profile was obtained for the biodistribution of cefuroxime in the brain, in which CLN showed a significantly higher Cmax, AUC0–t, prolonged half-life, and lower clearance as compared to free cefuroxime solution. Conclusion Overall, CLN showed excellent physicochemical properties, fulfilled the requirements for parenteral administration, and presented improved in vivo pharmacokinetic profile, which reflected its practical approach to enhance cefuroxime delivery to the brain.

Antiviral Nanodelivery Systems

Poor bioavailability of acyclovir in the treatment of viral infections remains one of the major drug delivery concerns of pharmaceutical manufacturers and researchers. Nanoparticulate systems have been exploited with the aim of improving the current pharmacological limitations of acyclovir administration. In fact, nanoparticles do offer many advantages, especially in terms of their physicochemical stability and sustained-release properties. Besides, they are made of biocompatible materials, which are nontoxic to cells. Acyclovir has been a focus since the last decade as one of the low bioavailability drug models loaded in various types of newly synthesized drug delivery vehicles. In this review, compositions and formulations of nanosized acyclovir particles, as well as their stability and pharmacokinetic profile, are discussed in further detail.