Formulation in vitro and in vivo evaluation of SRMS-based heterolipid-templated homolipid delivery system for diclofenac sodium.

The sole objective of this work was to design successful dosage oral forms of diclofenac sodium (DiNa)-loaded solid lipid microparticles (SLM) based on solidified reverse micellar solution (SRMS). Hot homogenization technique was employed to prepare DicNa SLM using a mixture goat fat and Phospholipon® 90 G as lipid matrix and Tween®-80 as mobile surfactant. Characterization based on percentage yield, morphology, particle size, zeta potential, percentage encapsulation, pH and stability of SLMs were investigated. Anti-inflammatory, gastrointestinal tract (GIT) sparing effect and pharmacokinetics were carried out in rat model after oral administration. Results showed that the SLMs were spherical and smooth. The optimized formulation (SLM-4) had particle size of 79.40 ± 0.31 µm, polydispersity index of 0.633 ± 0.190, zeta potential of -63.20 ± 0.12 mV and encapsulation efficiency of 91.2 ± 0.1% with good stability after 8 months of storage. The DicNa SLM had sustained release effect with good anti-inflammatory activity. Higher and prolonged plasma DicNa concentration was shown by the SLM-4 compared to pure drug and a conventional sample. These studies demonstrate that DicNa-loaded SLM based on SRMS could be a promising oral formulation for enhanced bioavailability, pharmacologic activity and gastrointestinal sparing effect of the NSAID, DicNa.

Some compaction characteristics of the hot water leaf extract og Nauclea latifiola: a potential antimalarial agent.

This study aims to develop a suitable tablet dosage form of Nauclea latifolia, a potential antimalarial agent. The compaction characteristics of the oven dried water extract were studied using the Heckel equation. The mechanical properties of the compacts were also determined. This preliminary information will be useful in developing a suitable dosage form of the extract for use in the management of malaria. The results showed that N. latifolia extract exhibited high densification due to dye filling while the subsequent rearrangement of the granules did not contribute, significantly, to their densification. The granules had enhanced plasticity as shown by the low yield point, Py. The tablets produced from the extract had good mechanical properties, with hardness increasing via compression pressure while the friability decreased. However, the tablets had poor disintegration properties; it is concluded that while tablets of suitable physical properties can be produced from the extract, a disintegrant would need to be included in the formulation to ensure adequate drug release.

Isolation and characterization of microcrystalline cellulose obtained from palm nut (elaeis guineensis) fibres

In this study; microcrystalline cellulose; coded MCC-PNF; was obtained from palm nut (Elaeis guineensis) fibres. MCC-PNF was examined for its physicochemical and powder properties. The powder properties of MCC-PNF were compared to those of the best commercial microcrystalline cellulose grade; Avicel PH 101. The extraction yield of MCC-PNF was approximately 8

Double-blind, placebo-controlled, randomised cross-over clinical trial of NIPRISAN in patients with Sickle Cell Disorder.

The study was undertaken to determine the safety and efficacy of NIPRISAN, a phytomedicine, developed for the management of patients with Sickle Cell Disorder (SCD). The study design is a placebo-controlled double blind cross-over trial. Eighty-two (82) patients with SCD were recruited and randomised into two groups. An initial 4 month pre-trial study was undertaken to determine the similarity of the groups. The main study was conducted over a twelve-month period with crossover at six months. Safety of the drug was assessed clinically and biochemically. NIPRISAN significantly (P < 0.01) reduced the frequency of SCD crisis associated with severe pains. Acute toxicity to the liver assessed by the activities of liver enzymes, indicate that NIPRISAN is safe. Renal function assessed by the serum levels of creatinine and blood urea nitrogen remained normal. Both the clinical and laboratory results of the present phase IIB (pivot) clinical study suggest that NIPRISAN is a safe and efficacious phytomedicine for the management of patients with Sickle Cell Disorder.

Some emulsifying and suspending properties of the mucilage extracted from kernels of Irvingia gabonensis.

The mucilage extracted from the kernels of Irvingia gabonensis was evaluated for use as suspending and emulsifying agent. The rheological behaviour of the mucilage was studied and compared to that of tragacanth. As a suspending agent, Irvingia mucilage was compared to tragacanth at various concentrations (0.5, 1.0, 1.5 and 2.0% w/v) in the formulation of sulphanilamide suspensions. At all concentrations the formulated suspensions with Irvingia mucilage gave higher Hu (final sedimentation height) and F (sedimentation volume) values. As an emulsifying agent, the properties of Irvingia mucilage was compared to tragacanth and acacia gum. The emulsions prepared with 0.6, 1.0, and 1.5% tragacanth and Irvingia 'cracked' within six days while that with 12.5% w/v acacia started showing signs of creaming at the tenth day. The emulsion prepared with 2.0% w/v Irvingia mucilage was however stable throughout the six weeks of study. The results indicate that Irvingia mucilage performed better than acacia and tragacanth even at lower concentrations in the formulation of emulsions and suspensions.