Recent advances in particulate anti-malarial drug delivery systems: A review

Malaria remains a tremendous health burden in tropical areas, causing a life-threatening disease and accounts for 1 to 2 million deaths round the globe yearly. Researchers have explored different novel approaches to deliver and improve the biopharmaceutical performance of drugs used in malaria chemotherapy. These novel drug delivery systems (NDDS) enhanced bioavailability of these drugs and also may offer controlled release of these drugs. The major aim of the NDDS is to improve the efficacy of these drugs, and at the same time to eliminate their toxicity. These NDDS include: micro/nanoparticulate DDS, emulsion based DDS, dendrimers and liposomes among others. The development of these particulate carriers as vehicles for the delivery of active compounds is a novel area of research that provides a new hope in malarial chemotherapy. The work presents various trends in malarial chemotherapy, as well as an exhaustive screening of different particulate drug delivery systems (PDDS) and the recent advances in the delivery of anti-malarial drugs using the novel particulate drug delivery systems (NPDDS)

Preliminary spectroscopic characterization of PEGylated mucin, a novel polymeric drug delivery system

The objective of this study was to evaluate, spectrophotometrically, the compatibility of non-mucinated polyethylene glycol (PEG) 4000 and non-PEGylated mucin in a PEGylated mucin matrices for drug delivery application. Mucin was extracted from the giant African land snails (Archachatina maginata) using chilled acetone and characterized in terms of qualitative properties and solubility profile. Polymeric matrices composed of PEG 4000 and mucin in ratios of 2:0 (A), 1:1 (B), 2:1(C) and 3:1 (D) were prepared by co-precipitation using chilled acetone. The matrices were characterized with respect to compatibility using the Fourier transform infrared (FT-IR) spectroscopy. Results of the qualitative tests performed on the snail mucin showed that carbohydrates, proteins and trace amounts of fats were present; the extracted mucin was light-brownish in colour, with a pleasant meaty odour. Snail mucin, when dispersed in water yielded a slightly viscous dispersion, but is not soluble in ethanol, acetone, 0.1 M sodium hydroxide, ammonium hydroxide and sulphuric acid. The presence of different peaks in the FT-IR spectra of the PEGylated mucin matrices compared with the non-PEGylated mucin (2:0) matrix and non-mucinated PEG 4000 (0:2) matrix indicated the formation of new polymers, which could be employed in drug delivery. This study has shown that PEGylation of mucin gives rise to new polymeric system with principal FT-IR peaks quite different from those of non-PEGylated mucin and nonmucinated PEG, and this may be employed in the delivery of drugs.Key words: PEGylation, drug delivery, mucin, Fourier transform infrared (FT-IR) spectroscopy, Archachatina maginata

Profiling the physicochemical and solid state properties of edible Tetracarpidium conophorum oil and its admixtures for drug delivery

The study is aimed at investigating the functional physicochemical and solid state characteristics of food-grade Tetracarpidium conophorum (T. conophorum) oil for possible application in the pharmaceutical industry for drug delivery. The oil was obtained by cold hexane extraction and its physicochemical properties including viscosity, pH, peroxide, acid, and thiobarbituric acid values, nutrient content, and fatty acid profile were determined. Admixtures of the oil with Softisan®154, a hydrogenated solid lipid from palm oil, were prepared to obtain matrices which were evaluated by differential scanning calorimetry, fourier-transform infrared spectroscopy, and x-ray diffractometry. Data from the study showed that T. conophorum oil had Newtonian flow behaviour, acidic pH, insignificant presence of hyperperoxides and malondialdehyde, contains minerals including calcium, magnesium, zinc, copper, manganese, iron, selenium, and potassium, vitamins including niacin (B3), thiamine (B1), cyanocobalamine (B12), ascorbic acid (C), and tocopherol (E), and long-chain saturated and unsaturated fatty acids including n-hexadecanoic acid, 9(Z)-octadecenoic acid, and cis-13-octadecenoic acid. The lipid matrices had low crystallinity and enthalpy values with increased amorphicity, and showed no destructive intermolecular interaction or incompatibility between T. conophorum oil and Softisan® 154. In conclusion, the results have shown that, in addition to T. conophorum oil being useful as food, it will also be an important excipient for the development of novel, safe, and effective lipid-based drug delivery systems

Novel Intravaginal Drug Delivery System Based on Molecularly PEGylated Lipid Matrices for Improved Antifungal Activity of Miconazole Nitrate

The aim of this study was to investigate the potential of microparticles based on biocompatible phytolipids [Softisan® 154 (SF) (hydrogenated palm oil) and super-refined sunseed oil (SO)] and polyethylene glycol- (PEG-) 4000 to improve intravaginal delivery of miconazole nitrate (MN) for effective treatment of vulvovaginal candidiasis (VVC). Lipid matrices (LMs) consisting of rational blends of SF and SO with or without PEG-4000 were prepared by fusion and characterized and employed to formulate MN-loaded solid lipid microparticles (SLMs) by melt-homogenization. The SLMs were characterized for physicochemical properties, anticandidal activity, and stability. Spherical discrete microparticles with good physicochemical properties and mean diameters suitable for vaginal drug delivery were obtained. Formulations based on SO:SF (1:9) and containing highest concentrations of PEG-4000 (4 %w/w) and MN (3.0 %w/w) were stable and gave highest encapsulation efficiency (83.05–87.75%) and inhibition zone diameter (25.87±0.94–26.33±0.94 mm) and significantly (p<0.05) faster and more powerful fungicidal activity regarding killing rate constant values (7.10 x 10−3–1.09 x 10−2 min−1) than commercial topical solution of MN (Fungusol®) (8.00 x 10−3 min−1) and pure MN sample (5.160 x 10−3 min−1). This study has shown that MN-loaded SLMs based on molecularly PEGylated lipid matrices could provide a better option to deal with VVC