EFFECT OF LYOPHILIZATION ON THE PHYSICOCHEMICAL AND PHYSICOTECHNICAL PROPERTIES OF ASPIRIN-LOADED LIPOSPHERES

Objectives: To formulate aspirin-loaded lipospheres and to study the effect of lyophilization on the physicochemical and physicotechnical properties.Materials and methods: Lipospheres were formulated using lipid matrix (LM) made from goat fat (70 %) and Phospholipon® 90H (30 %) by hot homogenization. The formulations were lyophilized and analysed for particle size and morphology, percent drug content (PDC), and in vitro drug release. The micromeritic properties of the formulations were also studied.Results and discussion: The unlyophilized lipospheres had particle size range of 35.9 ± 8.63 to 78.7 ± 3.30 μm, while the lyophilized formulations had particle size range of 16.6 ± 2.92 to 45.5 ± 2.72 μm. PDC of lipospheres ranged from 63.4 to 92 %. In vitro drug release showed about 92.4 and 91.3 % drug release at 5 h for A1 and B1lipospheres formulated with Poloxamer® 407 and Soluplus® respectively and containing 1 % of aspirin respectively, while 95 and 93 % was released at 8 h. The results of micromeritic studies showed that the lipospheres exhibited poor flowability.Conclusion: Lyophilized aspirin-loaded lipospheres showed good properties and could be used orally twice daily. Key words: Aspirin, lipids, micromeritic, lyophilization, NSAIDsÂ

ARTEMETHER LUMEFANTRINE LOADED LIPOSPHERES EVALUATION OF PROPERTIES OF SOLUTOL HS 15 AND SOLUPLUS ON THE IN VITRO PROPERTIES

To formulate artemether lumefantrine loaded lipospheres and to evaluate the effect of excipients on the in vitro properties  Materials and methods: Lipospheres were formulated using goat fat (70 percentage) and Phospholipon 90H (70 percentage) as the lipid matrix, Solutol HS 15 and Soluplus were used respectively as surfactants.  The lipospheres were formulated by melt homogenization and analysed for drug content, encapsulation efficiency (EEpercentage), particle size and pH stability. In vitro release was studied in simulated gastric fluid (SGF, 1.2) and simulated intestinal fluid (SIF, 7.2).       Results: Lipospheres formulated with Solutol had particle size range of 24.16 to 30.89 μm, while those formulated with Soluplushad particle size range of 24.72 to 74.16 μm. The formulations showed a decline in pH at 30 days. The EE of artemether range from 71.80 to 75.30 percentage for lipospheres formulated with Soluplus, while those formulated with Solutolhad EEpercentage of 65.30 to 75.02 percentage. Also, the EEpercentage of lumefantrine ranged from 76.36 to 88.99 percentage for lipospheres formulated with Soluplus, while those containing Solutolhad EE range of 73.22 to 85.06 percentage. Formulations exhibited sustained release properties with maximum release of at 6 h, however, lumefantrine exhibited higher release than artemether in SIF (p less than 0.05) and significantly lower release in SGF (p less than 0.05).                                                                                                                                           Conclusion: Lipospheres exhibited good properties as a delivery system for artemether-lumefantrine. Keywords: Goat fat, phospholipid, antimalaria, melt homogenization, loading capacit

Evaluation of binder and disintegrant properties of starch derived from Xanthosoma sagittifolium in metronidazole tablets

The aim of the study was to formulate metronidazole tablets using starch from Xanthosoma sagittifolium as binder and disintegrant in metronidazole tablets. Metronidazole tablets were produced by wet granulation method using X. sagittifolium starch as binder at concentrations of 5, 10, 15 and 20% w/w, and as disintegrant (5% w/w). The micromeritic properties of the granules were determined using the direct and indirect methods. The necessary official and non official tests were performed on the tablets to include uniformity of tablets weight, content of active ingredient, disintegration test, hardness, friability tests and in vitro drug release. Also, the phytochemical constituents of the starch were determined. The results show that the granules had a good flow and values obtained were within the specified limits for the production of good quality tablets. Deviations obtained from the tablet weight uniformity test were significantly (p< 0.05) below 5%. Tablets disintegration time ranged from 3.00 ± 0.08 min to 14.00 ± 0.10 min for M1 and M4 tablets formulated with 5 and 20% of X. sagittifolium starch respectively. The tablets hardness ranged from 7.20 ± 1.25 to 8.55 ± 1.17 kgf. In vitro release showed that M1 tablets had T25, T50 and T90 % at 5, 13 and 23 min respectively, while M4 tablets had T25, T50 and T90 % at 8, 18 min and were unable to release 90% of metronidazole at 30 min. Phytochemical analysis showed that the starch contained alkaloids, glycosides, carbohydrate and steroids. Therefore, starch from X. sagittifolium could be used to formulate metronidazole tablets for improved oral bioavailability of metronidazole.Keywords: Xanthosoma sagittifolium starch, tablets binder and disintegrant, metronidazoleAfrican Journal of Biotechnology Vol. 12(20), pp. 3064-307

FORMULATION AND EVALUATION OF ETHANOLIC EXTRACT OF CRYPTOLEPIS SANGUINOLENTA ROOT TABLETS

Objectives: To study were to formulate the ethanolic extract of Cryptolepis sanguinolenta root into tablets and to evaluate the effect of different binders and binder concentration on the properties of tablets. Materials and method: The phytochemistry of ethanolic extract of Cryptolepis sanguinolenta was evaluated. The tablets were formulated by wet granulation 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 necessary official and unofficial tests. Results: Phytochemical analysis revealed the presence of alkaloids, terpenoids, steroids, proteins, carbohydrate, resins, reducing sugars and glycosides. Tannins, saponins, flavonoids and acidic compounds were absent.  The tablets passed the uniformity of weight test and deviations obtained complied with BP specifications. Tablets disintegration time ranged from 8.00 ± 0.10 to 13.50 ± 0.21 min for tablets formulated with 2 and 4 % gelatin and 10.00 ± 0.17 to 31.00 ± 0.27 min for tablets formulated with 2 and 8 % SCMC. C. sanguinolenta tablets formulated gelatin significantly showed higher hardness values than SCMC (p < 0.05). Tablets showed friability of approximately ≤ 1 %. Conclusion: Therefore, gelatin showed good properties for formulating Cryptolepis sanguinolenta normal release tablets than SCMC.Â

Biochemical, rheological and hydrophile-lipophile balance (HLB) evaluation of Archachatina marginata (snail) mucin extract for possible nutraceutical and nano biopharmaceutical applications

Purpose: To evaluate the rheological, biochemical, hydrophile-lipophile balance (HLB) of Archachatina marginata (snail) mucin extract for possible use as a nutraceutical and nano biopharmaceutical material. Methods: Snail mucin was extracted with acetone and water, lyophilized and the biochemical, proximate and mineral analyses of the extracts were studied using standard methods. The rheological properties of the extracts (1, 2, 4 and 8 % w/v) and their emulsion-based preparations were evaluated. Other physicochemical properties and HLB values of the preparations were also determined. Results: Snail mucin extracts contained protein (84 %), fats (2.91 %) and carbohydrate (1.2 %) and showed significant nutraceutical composition (p < 0.05). Ash content of 4.21 and 4.12 % was obtained for water and acetone extracts, respectively. Moisture content was < 9 % for both the aqueous and nonaqueous mucin extracts. Potassium, calcium and phosphorus were present in high quantities in the extracts while iron, copper and zinc were in trace amounts (< 4 %). Mucin dispersions exhibited viscosity in the range of 0.89 to 0.93 cp. Water sorption and dry weight were higher in the acetone extract than in the aqueous extract. The HLB values, which ranged from 7 to 15, were within the acceptable values for material for nanobiopharmaceutical application, except that the acetone extract. Conclusion: Snail mucin exhibits good nutraceutical properties and also possesses good properties that render it a potential excipient for use in the formulation of drug delivery system

Solid self-emulsifying drug delivery system based on a homolipid and vegetable oil: A potential vehicle for the delivery of indomethacin a disadvantaged drug

Background: The successful utility of some biocompatible natural excipients may be more advantageous over their synthetic counterparts in drug formulations. Indomethacin is a potent non-steroidal anti-inflammatory drug disadvantaged by adverse effects. Aim: Hence, the aim of this study was to formulate indomethacin-based solid self-emulsifying drug delivery system (SSEDDS) for possible improvement on aqueous solubility and anti-inflammatory property of indomethacin using two biocompatible lipid excipients. Materials and Methods: Indomethacin-loaded SSEDDS were formulated with Bos indicus (BI) fat or its blend with Pentaclethra macrophylla oil. The surfactant component constituted of Tween 65 and Tween 80 blend while Span 85 served as the co-surfactant. Carbosil® was incorporated in some of the formulations as a viscosity enhancer and stabilizer. The following in vitro properties of the formulations were studied: visual isotropicity test, droplet size, emulsification time, aqueous dilution and drug precipitation, drug content, and drug release studies respectively. The anti-inflammatory properties were also studied in Wistar rats. Statistical Analysis: Results were presented as the mean ± standard deviation. One-way analysis of variance was used to determine statistical significance using the Statistical Package for the Social Sciences (SPSS), version 13.0 (SPSS Inc. U.S.A). P 0< 0.05 was considered statistically significant. Results: All batches were isotropic before and after drug loading. Batches containing BI fat and PM oil blend exhibited faster emulsification time (P < 0.05) than those formulated with only BI fat. Carbosil® significantly ( P < 0.05) increased the emulsification time. Faster drug release occurred in batches with oil blends. Higher significant ( P < 0.05) anti-inflammatory effect was demonstrated by indomethacin self-emulsifying drug delivery system compared to the reference indomethacin powder. Therefore, BI fat and PM oil have proved useful lipid excipients in achieving improved solubility and increased anti-inflammatory activity of indomethacin

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 size and 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 μm. 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-inflammatory properties 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