In vitro and In vivo Characterisation of Piroxicam-Loaded Dika Wax Lipospheres

Purpose: To formulate piroxicam-loaded lipospheres and evaluate their in vitro and in vivo properties.Method: Piroxicam-loaded lipospheres were prepared by hot  homogenization technique using dika wax and Phospholipon® 90G (1:1, 1:2 and 2:1) as the lipid matrix. Characterisation, based on particle sizeand morphology, pH, drug content and encapsulation efficiency, were carried out on the lipospheres. In vitro release was evaluated in simulated intestinal fluid (pH 7.5). Anti-inflammatory and ulcerogenic properties of the piroxicam-loaded lipospheres were studied using healthy, adult Wistar rats.Result: Photomicrographs revealed spherical particles in the range of 1.66 – 3.56 ìm. The results also indicated that lipospheres formulated with lipid matrix 1:1 and containing 0.25 % piroxicam had the highest encapsulation efficiency of 84 %. In vitro release data showed that lipospheres formulated with lipid matrix having higher concentration of dika wax exhibited the fastest drug release of drug with maximum release time between 60 - 70 min. The lipospheres exhibited good anti-inflammatoryproperties with 58.6 % oedema inhibition at 5 h. Piroxicam-loaded liposheres had an ulcer index of zero while, the reference (plain piroxicam) had an ulcer index of 15.00 ± 1.23 (p < 0.05).Conclusion: Piroxicam lipospheres formulated with a mixture of dika wax and phospholipid exhibited good in vitro and in vivo properties.Keywords: Dika wax, Lipospheres, Piroxicam, Phospholipid, Ulcerogenicity, Anti-inflammator

Solidified Reverse Micellar Solution (SRMS)-Based Indomethacin Sustained-Release Tablets: Formulation and In vitro Evaluation

Purpose: To formulate and evaluate sustained-release indomethacin tablets based on solidified reverse micellar solution (SRMS).Methods: SRMS consisting of mixtures of phospholipid (Phospholipon® 90H) and triglyceride (Softisan® 154) were prepared in the ratios of 1:1, 2:1 and 1:2, respectively. SRMS-based tablets containing 75 mg of indomethacin each were prepared using a validated plastic mould. The physicochemical properties of the tablet formulations were studied. In vitro release study was carried out in simulated intestinal fluid (SIF, pH 7.5).Results: The results showed that the physicochemical properties of the tablet formulations were significantly affected by the composition/ratio of the lipid matrix used (p < 0.05). Tablet hardness ranged from 5.00 ± 0.39 to 5.60 ± 0.36 kgf for tablets formulated with SRMS 1:2 and 2:1 (N3 and N2), respectively. The tablets exhibited friability of < 1 % (p < 0.05). Erosion time in SIF ranged from 124.0 ± 0.5 to 180.0 ± 1.1 min while drug release from the tablets reached a maximum in 8 – 11 h for all thebatches.Conclusion: Indomethacin tablets based on SRMS exhibited good sustained-release properties and can be further developed to achieve once daily administration for improved patient adherence to therapy.Keywords: Solidified reverse micellar solution, Phospholipid, Triglyceride, Indomethacin, Sustained release

PHYTOSOMES ENHANCED THE ANTIBACTERIAL AND ANTIFUNGAL PROPERTIES OF LANTANA CAMARA

Aim: The aim of the work was to formulate Lantana camara phytosomes to improve the antimicrobial properties. Methods: L. camara phytosomes were prepared by solvent evaporation using soy lecithin (Phospholipon® 90H). The effect of surfactant Poloxamer 188 was carried out. The qualitative and quantitative analysis of the phytoconstituents was analyzed. The encapsulation efficiency and loading capacity were studied. Furthermore, the in vitro release profile was studied in ethanolic buffer. The inhibition zone diameter (IZD) was evaluated against three bacterial and two fungi. Results: The results showed that saponins were the most dominant phytochemical with about 7% on the plant leaves. The highest EE of 82.80% was obtained. In vitro release showed about 23% drug release at 60 min. The IZD results showed that L. camara had significantly higher activity against Escherichia coli and Listeria ivanovii than Staphylococcus aureus (p<0.05). The results also showed that for Candida albicans, L. camara phytosomes had significantly higher IZD than the extract (p<0.05). However, the L. camara extract and the formulations showed no activity against the Aspergillus flavus. Conclusions: Phytosomes enhanced the antimicrobial properties of L. camara and could serve as a good delivery system for this herbal drug

FORMULATION AND EVALUATION OF NOVEL HERBOSPHERES DELIVERY SYSTEM OF LEAF EXTRACT OF VERNONIA AMYGDALINA DEL (ASTERACEAE)

Objectives: The objectives of the study were to formulate herbospheres of V. amygdalina leaf-extract and to study the in vitro and antibacterial properties of the formulationsVernonia amygdalina, Del (Asteraceae) is a tropical shrub used throughout West Africa for the management of diabetes and other metabolic diseases associated with the liver. The plant has acquired special relevance recently, having been proved in human medicine to possess potent antimalarial, antihelmintic, and antitumorigenic properties.Methods: Herbospheres were formulated with lipid matrices consisting of goat fat (70%) and Phospholipon® 90H (30%) by melt homogenization and characterized for taste masking, particle size, pH, encapsulation efficiency, and loading capacity. Inhibition zone diameter of the herbospheres was studied.Results: Phytochemical analysis showed the presence of alkaloids, saponins, tannins, carbohydrates, reducing sugars, protein, steroids, flavonoids, and cardiac glycosides in substantial quantities. Acid compounds and oils were, however, absent. The particle size of herbospheres ranged from 6.90±0.2 to 28.50±0.71 μm and was significantly affected by the type of surfactant used (p < 0.05). The pH ranged from 5.6 to 5.9 at day 1 and 4.1 to 4.4 at 30 days. Highest EE of 90–92 % was obtained and was significantly affected by surfactant used (p<0.05). Formulations exhibited significantly higher inhibition of Staphylococcus aureus than tetracycline pure sample used as the reference drug (p<0.05).Conclusion: V. amygdalina herbospheres formulations had antibacterial properties in addition to taste masking and high encapsulation of the extract

Formulation and Release Characteristics of Zidovudine-Loaded Solidified Lipid Microparticles

Purpose: To formulate and determine the release profile of zidovudine (AZT)-loaded solidified lipid microparticles (SLMs).Methods: Different concentrations (0, 1, 2, 3 and 5 %w/w) of zidovudine (AZT) were formulated into microparticles in melt dispersion of Phospholipon® 90H and goat fat in the ratio 1:1, 2:1, 2:3 and 1:3 followed by lyophilization. They were characterized for particle size, yield, entrapment efficiency (EE) and loading capacity (LC). In vitro release kinetics and mechanism of release were assessed sequentially in simulated gastric fluid (SGF, pH 1.2)and simulated intestinal fluid (SIF, pH 7.2).Results: The ratio 1: 1 formulation was the most stable in terms of physical observation.. Particle size analysis indicated that the particles were irregular in shape with size ranging from 5.10 ± 0.10 to 13.40 ± 2.20 μm. Yield decreased with increase in drug concentrations in the SLMs formulations. EE data showed that the microparticles containing 1 % w/w of AZT had the highest entrapment efficiency of 74.0 ± 0.03 %. LC also decreased with increase in concentration of AZT. AZT tablet released most of its content within 5 min with a sharp decrease in the concentration but the SLMs maintained its release for 8 to 12 h in different batchesConclusion: The results show that drug content has influence on drug release from the SLMs, but not on the mechanism of release. Furthermore, dose dumping was avoided and drug release mechanism was mostly non-Fickian while for the reference (commercial) tablet, it was Fickian.Keywords: Phospholipon® 90H, Solidified lipid microparticles, Solidified reverse micellar microparticle, Zidovudine

Cryptolepis sanguinolenta Root Tablets: Effect of Binder Type and Concentration on the Tablet Properties

ABSTRACT The objectives of the study were to formulate Cryptolepis sanguinolenta root powder into tablets and to evaluate the effect of different binders and binder concentrations on the properties of tablets. The tablets were formulated by the wet granulation method using gelatin and sodium carboxymethyl cellulose (SCMC) as binders at concentrations of 2%, 4%, 6% and 8%w/w. The tablets were evaluated using the relevant official and unofficial tests. Also the phytochemistry of the powdered root extract of C. sanguinolenta was evaluated. Phytochemical analysis showed that C. sanguinolenta root contains alkaloids, terpenoids, steroids, proteins, carbohydrate, resins, reducing sugars and glycosides. Tablets formulated with SCMC significantly exhibited higher disintegration times than those formulated with gelatin (p<0.05).Tablets hardness ranged from 3.51 ± 0.12 to 5.02 ± 0.10 kgf for A1 and A4 tablets formulated with 2 and 8% gelatin and 2.00 ± 0.11 to 5.00 ± 0.17 kgf for B1 and B4 tablets formulated with 2 and 8% SCMC. All the tablet batches exhibited friability of < 1% (p<0.05). Therefore the powdered root of C. sanguinolenta could be formulated as normal release tablets using gelatin and SCMC in order to standardize the preparation and also enhance patient's compliance

Evaluation of Gentamicin-Entrapped Solid Lipid Microparticles Formulated with a Biodegradable Homolipid from Capra hircus

Purpose: To formulate solidified reverse micellar solutions (SRMS)-based solid lipid microparticles (SLMs) using homolipid from Capra hircus, and evaluate its suitability for the delivery of gentamicin.Methods: SLMs were formulated by melt-emulsification using SRMS (15 % w/w Phospholipon® 90G in 35 % w/w Capra hircus), PEG 4000 and  gentamicin (1.0, 2.0 and 3.0 % w/w), and characterized with respect to size, morphology, encapsulation efficiency (EE) and pH-dependent stability. In vitro release of gentamicin from the SLMs was performed in phosphate buffer (pH 7.4) while bioevaluation was carried out using clinical isolates of Pseudomonas aeruginosa and Staphylococcus aureus.Results: Stable and discrete SLMs of size range 1.47 ± 0.02 to 3.55 ± 0.09 µm were obtained. The SLMs showed a biphasic pattern of drug release and exhibited time-dependent and capacity-limited bioactivity. Overall, SLMs containing 2 % w/w SRMS, 3 % w/w gentamicin and PEG 4000 entrappedthe highest amount of drug, released 99 % of drug and gave the highest inhibitory zone diameter (IZD) against the organisms within 420 min, while plain gentamicin gave the least.Conclusion: SRMS-based SLMs prepared with homolipid from Capra hircus offers a suitable delivery system for gentamicin.Keywords: Solid lipid microparticles, Gentamicin, Capra hircus,   Phospholipon® 90 G, Solidified reverse micellar solutio