IN VITRO PROPERTIES OF SOLID LIPID MICROPARTICLES (SLMS) LOADED WITH METHANOLIC EXTRACT OF GARCINIA KOLA (HECKEL) SEED

Objective: The decline in the use of herbal medicine especially in the Western world may be due to lack of readily available market brand formulations and the fact that most herbal remedies are taken as tea, decoctions and infusions. The taste of some of these herbal drugs is not palatable, and some have unpleasant odour and colour hence, the need to formulate these drugs in form of encapsulated dosage forms. The objective of the work was to formulate solid lipid microparticles (SLMs) loaded with the methanolic extract of Garcinia kola seed. Methods: The SLMs containing 1 and 3 % of Garcinia kola seed extract were formulated using fat from Capra hircus and Phospholipon® 90H (3:1). The particle morphology and size, encapsulation efficiency (EE%), pH, in vitro release and the inhibition zone diameter (IZD) of the SLMs were determined. Results: The results showed that the extract was very bitter while, the encapsulated G. kola had slight bitter taste. The pH remained in the acidic region from 1 to 30 days. Particle size of 28.65 ± 1.13 and 29.49 ± 1.24 µm were obtained for SLMs loaded with 1 and 3 % of the extract respectively. SLMs had high EE% of 94 % and also exhibited good release of the extract in simulated intestinal fluid (SIF, pH 7.2). Garcinia kola-loaded SLMs had good activity against Staphylococcus aureus and no action against Escherichia coli. Conclusion: Therefore, Garcinia kola seed extract could be formulated as SLMs in order to mask its bitter taste and improve compliance. Â

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

Development of Transdermal Patches for the Delivery of Chlorpheniramine in Infants using Hypromellose and Cassava Starch Composite Polymers

Background: Chlorpheniramine is an antihistamine that is used in the treatment of rhinitis and other allergies. Objectives: The objectives of this research was to develop and evaluate transdermal patches for improved delivery of chlorpheniramine in infants using hypromellose and cassava starch composite polymers. Methods: Chlorpheniramine transdermal patches were formulated by solvent casting method using varying amounts of hypromellose (hydroxypropyl methylcellulose), cassava starch and polyethylene glycol 4000. The formulated transdermal patches were characterized by Fourier Transform Infra-red Spectroscopy (FT-IR), folding endurance, elongation breaking test, percentage moisture uptake/loss and ex vivo permeation studies. Results: The spectra showed no chemical interaction between the ingredients. The transdermal patches showed elastic qualities and high folding endurance. Patches with consistently high moisture uptake (around 40%) were observed to contain high concentration of cassava starch while those with higher amounts of HPMC lost more water (around 35%). The ex vivo study showed efficient permeation and flux for the target purpose. Conclusion: Transdermal patches may be used to deliver low dose chlorpheniramine drug through the skin possibly soft and thin infant skin. Keywords: Transdermal; permeation; flux; allergy; chlorpheniramin

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

Formulation and characterization of artemether-loaded sodium alginate microcapsules

Purpose: To increase the solubility of artemether (ART) in Transcutol® HP through microencapsulation in sodium alginate polymer to achieve  sustained in vivo release.Method: Graded concentrations of ART (0.00, 0.25, 0.50, 0.75, and 1.00 g) microcapsules were produced using Tween® 80 by the cold  homogenization method at 24 x 1000 rpm for 15 min. Characterization based on yield, encapsulation efficiency (EE), particle size, pH stability,  differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR) and in vivo release using Peter’s four-day suppressive protocol in Wistar mice infected with Plasmodium berghei, were determined.Results: The results obtained indicate that 0.5 g ART-loaded microcapsules (AMC) showed the highest yield of 96.85 %. The EE of 88.3 %  corresponded to 0.75 g ART-loaded microcapsules. DSC results revealed that there was a significant reduction in enthalpy in all the formulations compared to the crystalline drug, but no strong bond interaction occurred except for the blank microcapsules. The AMC1.0 showed high dose-dependent plasmodial growth inhibition of 88.75 % while AMC0.25 had the least (68.13 %).Conclusion: The artemether microcapsules showed sustained release characteristics for oral delivery of artemether and therefore may reduce some of the adverse effects associated with high dose artemether therapy in conventional oral tablets. Keywords: Malaria, Artemether, Transcutol® HP, Sustained-release, RBC count, Antiplasmodial activit

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

Studies on the Charge-TransferInteraction Between TamoxifenCitrate and Chloranilic Acid: Charge-transfer between tamoxifen and chloranilic acid

The complex formed as a consequence of the interaction between the electron-acceptor P-chloranilic acid and an electron donor tamoxifen citrate was employedin the assay of the drug in pure powder and tablets. Chloranilic acid was found toform a charge-transfer complex in a 1:1 stoichiometric ratio, with tamoxifen citrate.The wavelength of maximum absorption for the complex was found to be 550 nmwhile the absorbance was linear over the concentration range of 2-100 g/ml.Evaluations of the various thermodynamic parameters by means of the Scottequation was carried out and were found to decrease with increase in temperature.The free energy change (ΔG°) and the enthalpy of formation (ΔH°) as well as theentropy (ΔS°) were determined for various interactions. Results obtained suggestthat the proposed method may be conveniently applied in the analysis ofcommercially available tamoxifen citrate tablets with a high degree of accuracy andreproducibility

Formulation and in vitro characterization of piroxicam solid lipid microparticles for topical application

Swollen body parts or edema is a condition characterized by increased accumulation of fluid. The aim of this research is to develop a delivery system capable of facilitating improved and controlled topical delivery of piroxicam during high energy activities, including sports. Irvingia fat was extracted from the nut of Irvingia gabonensis var. excelsa (Irvingia wombolu) with petroleum ether (40-60 °C) and analyzed using gas chromatography-mass spectrometry (GC-MS). The extracted fat and its lipid matrices with Phospholipon®90G (P90G) (with and without piroxicam) were characterized by differential scanning calorimetry (DSC) and small angle X-ray diffraction (SAXD). Piroxicam solid lipid microparticles (SLM), based on the extracted lipid, were formulated by hot homogenization and characterized by drug encapsulation efficiency (EE), particle size, yield and dispersion pH. Drug release and diffusion studies were performed for the SLM dispersions using dialysis membrane. The GC-MS indicated presence of C12-C18 fatty acids. The DSC thermograms of the piroxicam-loaded lipid matrices showed melting point of 41 °C, whereas reduced enthalpy and crystallinity were observed in the presence of P90G. The EE of the SLMs were above 98 and particle sizes around 10 µm. Piroxicam SLM dispersions formulated with lipid matrices consisting 3:1 irvingia fat/ P90G had the highest drug diffusion across the membrane. Therefore, solid lipid microparticles based on irvingia fat-P90G structured matrices can be used to improve loading, controlled diffusion, and possibly, overall topical performance of piroxicam.