Solid lipid nanoparticle (SLNs) formulae were utilized for the release of 5-flurouracil (5-FU) inside the colonic medium for local treatment of colon cancer. SLNs were prepared by double emulsion-solvent evaporation technique (w/o/w) using triglyceride esters, Dynasan™ 114 or Dynasan™ 118 along with soyalecithin as the lipid parts. Different formulation parameters; including type of Dynasan, soyalicithin:Dynasan ratio, drug:total lipid ratio, and polyvinyl alcohol (PVA) concentration were studied with respect to particle size and drug entrapment efficiency. Results showed that formula 8 (F8) with composition of 20% 5-FU, 27% Dynasan™ 114, and 53% soyalithicin and F14 (20% 5-FU, 27% Dynasan™ 118, and 53% soyalithicin), which were stabilized by 0.5% PVA, as well as F10 with similar composition as F8 but stabilized by 2% PVA were considered the optimum formulae as they combined small particle sizes and relatively high encapsulation efficiencies. F8 had a particle size of 402.5 nm ± 34.5 with a polydispersity value of 0.005 and an encapsulation efficiency of 51%, F10 had a 617.3 nm ± 54.3 particle size with 0.005 polydispersity value and 49.1% encapsulation efficiency, whereas formula F14 showed a particle size of 343 nm ± 29 with 0.005 polydispersity, and an encapsulation efficiency of 59.09%. DSC and FTIR results suggested the existence of the lipids in the solid crystalline state. Incomplete biphasic prolonged release profile of the drug from The three formulae was observed in phosphate buffer pH 6.8 as well as simulated colonic medium containing rat caecal contents. A burst release with magnitudes of 26%, 32% and 28.8% cumulative drug released were noticed in the first hour samples incubated in phosphate buffer pH 6.8 for both F8, F10 and F14, respectively, followed by a slow release profile reaching 50%, 46.3% and 52% after 48 hours.
An isocratic simple rapid assay has been developed and validated for the determination of carbamazepine (CBZ) in both solution form and rabbit plasma using propylparaben as an internal standard. The assay was performed using a μ-Bondapak C18 (150 mm × 4.6 mm i.d) with a mobile phase consisting of methanol and water (50:50), the flow rate was 1 ml/min and UV detection at 285 nm. The method was found to be specific for CBZ, no interfering peaks were observed with an overall analytical run time of 15 min. Accuracy reported as % recovery were found to be 98.37-100.45% and 97.53-103.58% for inter-day and intra-day accuracies, respectively. Inter-day precision (reproducibility) was found to be 0.53-2.75% RSD, while intra-day precision (repeatability) was found to be 1.06-3.7% RSD for the samples studied. The calibration curve was found to be linear with the equation y = 0.2847x + 0.0138, with a correlation coefficient of 0.9999 (R (2)) over a concentration range of 0.5-40 μg/ml. The limit of quantitation was the lowest concentration. The method is simple and rapid and does not require any preliminary treatment of the sample. The method was fully validated.
A simple isocratic stability-indicating high-performance liquid chromatographic method with UV detection using thymine as an internal standard is developed. The method is validated and the degradation products are determined. The method is applied for the assessment of the stability of 5-fluorouracil in rat caecal content as a simulated colon medium under anaerobic conditions. The drug decomposes under acidic, alkaline, thermal, and oxidative stress. The drug is highly susceptible to acidic, alkaline, and oxidative hydrolysis as compared to alkaline conditions. Separation of the drug from major and minor degradation products is successfully achieved on a C(18) analytical, micro-bondapak column. The detection wavelength is 260 nm. The method is validated, and the response is found to be linear in the drug concentration range of 0.1-2.0 microg/mL. The high linearity of the standard calibration curve of 5-fluorouracil in the rat content is found to be R(2) = 0.998 in the concentration range from 0.5 to 5 microg/mL. No degradation occurred after incubation of 5-fluorouracil in the rat caecal contents. The standard deviation and coefficient of variation values for intra- and inter-day precision study exhibit acceptable accuracy and precision data throughout the concentration range investigated.
Itraconazole (ITZ) solid complex using hydroxypropyl-beta-cyclodextrin (ITZ-HP-beta-CD) with 20% polyvinylpyrrolidone was prepared by a co-evaporation method. The complex improved antifungal activity against C. parapasilosis and C. albicans. The complex demonstrated good flow and compressibility characteristics. The complex was formulated as a capsule dosage form and drug release was evaluated. Capsules containing ITZ-HP-beta-CD at a molar ratio of 1:3 with 20% polyvinylpyrrolidone have a faster dissolution rate than commercial capsules (Sporanox). About 88% of ITZ was released in less than 30 min and the initial dissolution rate exhibited a 3.5-fold increase compared to the commercial product. UV spectrophotometeric, HPLC, and antimicrobial methods were used to determine ITZ concentration in the release medium and the results obtained by these methods are reported. It was found that HPLC analysis is a suitable and reliable method for determination of the drug concentration with a coefficient of variation less than 10%. The intraday precision showed a coefficient of variation less than 3.96%, and that for interday was less than 4.99%. The HPLC method was more accurate and precise than the antimicrobial and UV-spectrophotometric methods for determination of ITZ concentration present in the release medium.
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