Nanovesicle Formulation Enhances Anti-inflammatory Property and Safe Use of Piroxicam.

BACKGROUND: Enhanced utilization of certain drugs may be possible through the development of alternative delivery forms. It has been observed that NSAIDs have adverse gastrointestinal tract effects such as irritation and ulceration during anti-inflammatory therapy. This challenge may be overcome through nano topical formulations. OBJECTIVE: This study aimed to explore the potentials of a transdermal nanovesicular formulation for safe and enhanced delivery of piroxicam (PRX), a poorly water-soluble NSAID. METHODS: Preformulation studies were conducted using DSC and FTIR. Ethosomal nanovesicular carrier (ENVC) was prepared by thin-film deposition technique using Phospholipon® 90 H (P90H) and ethanol and then converted into gel form. The formulation was characterized using a commercial PRX gel as control. Permeation studies were conducted using rat skin and Franz diffusion cell. Samples were assayed spectrophotometrically, and the obtained data was analyzed by ANOVA using GraphPad Prism software. RESULTS: The preformulation studies showed compatibility between PRX and P90H. Spherical vesicles of mean size 343.1 ± 5.9 nm, and polydispersity index 0.510 were produced, which remained stable for over 2 years. The optimized formulation (PE30) exhibited pseudoplastic flow, indicating good consistency. The rate of permeation increased with time in the following order: PE30 > Commercial, with significant difference (p< 0.05). It also showed higher inhibition of inflammation (71.92 ± 9.67%) than the reference (64.12 ± 7.92%). CONCLUSION: ENVC gel of PRX was formulated. It showed potentials for enhanced transdermal delivery and anti-inflammatory activity relative to the reference. This may be further developed as a safe alternative to the oral form.

Nanovesicular carriers as alternative drug delivery systems: ethosomes in focus.

INTRODUCTION: The application of vesicular carrier formulations has generated promise of overcoming some problems associated with drug delivery arising from not only the physicochemical properties of the drug but also those of the biological barriers, such as the membrane linings of various body tissues and the skin. This review article discusses the importance of various vesicular carriers, namely liposomes, niosomes, transfersomes and ethosomes in drug delivery with greater emphasis on ethosomes. AREAS COVERED: The nature, mechanism of drug delivery, methods of preparation as well as characterization of vesicular carriers was discussed with a focus on ethosomes. An overview of their potential applications was provided with discussions on the future prospects and challenges of achieving enhanced drug delivery using ethosomes. EXPERT OPINION: Vesicular carriers offer controlled and sustained drug release, improved permeability and protection of the encapsulated bioactives. Ethosomes offer more efficient and enhanced bioavailability better than the older dosage forms owing to the high ethanol content. Ethosomes have potential applications in the development of nanomedicines, including phytomedicines, for the treatment of challenging diseases ravaging the world today. The future holds great prospects in the utilization of vesicular carriers, especially ethosomes, in overcoming peculiar problems of drug delivery.

New direct compression excipient from tigernut starch: physicochemical and functional properties.

Tigernut starch has been isolated and modified by forced retrogradation of the acidic gel by freezing and thawing processes. Relevant physicochemical and functional properties of the new excipient (tigernut starch modified by acid gelation and accelerated (forced) retrogradation (ST(AM))) were evaluated as a direct compression excipient in relation to the native tigernut starch (ST(NA)), intermediate product (tigernut starch modified by acid gelation (ST(A))), and microcrystalline cellulose (MCC). The particle morphology, swelling capacity, moisture sorption, differential scanning calorimeter (DSC) thermographs and X-ray powder diffraction (XRD) patterns, flow, dilution capacity, and tablet disintegration efficiency were evaluated. The particles of ST(NA) were either round or oval in shape, ST(A) were smooth with thick round edges and hollowed center while ST(AM) were long, smooth, and irregularly shaped typically resembling MCC. The DSC thermographs of ST(NA) and MCC showed two endothermic transitions as compared with ST(A) and ST(AM) which showed an endothermic and an exothermic. The moisture uptake, swelling, flow, and dilution capacity of ST(AM) were higher than those of MCC, ST(A), and ST(NA). The XRD pattern and moisture sorption profile of ST(AM) showed similarities and differences with ST(NA), ST(A), and MCC that relate the modification. Acetylsalicylic acid (ASA) tablets containing ST(AM) disintegrated at 3±0.5 min as compared with the tablets containing ST(NA), ST(A), and MCC which disintegrated at 8.5±0.5, 10±0.5, and 58±0.8 min, respectively. The study shows the physicochemical properties of tigernut starch modified by forced retrogradation as well as its potential as an efficient direct compression excipient with enhanced flow and disintegration abilities for tablets production.

In vivo antiplasmodial activities of aqueous extract of Bridelia ferruginea stem bark against Plasmodium berghei berghei in mice.

CONTEXT: Bridelia ferruginea Benth (Euphorbiaceae) is an indigenous medicinal plant in Nigeria. It is usually a gnarled shrub which sometimes reaches the size of a tree in suitable condition. Decoctions of parts of this plant have been employed in ethno medicine in many parts of Africa for treatment of many ailments including malaria fever. OBJECTIVE: In vivo antiplasmodial activity of aqueous stem bark extract of BF was investigated against Plasmodium berghei-infected mice. MATERIALS AND METHODS: The aqueous stem bark extract of BF (100-400 mg/kg) was administered orally to P. berghei-infected mice in both early and established models of antiplasmodial studies. RESULTS: The extract exhibited significant (p < 0.05) antiplasmodial activity in early and established infection tests with a considerable mean survival time comparable to that of chloroquine, 10 mg/kg. The oral LD(50) obtained was greater than 5000 mg/kg in mice. DISCUSSION AND CONCLUSIONS: The findings show that aqueous stem bark extract of Bridelia ferruginea possesses considerable antiplasmodial activity which can be developed in malaria therapy.