Continuous Melt Granulation for Taste-Masking of Ibuprofen

Taste-masking of drugs, particularly to produce formulations for pediatric patients, can be challenging and require complex manufacturing approaches. The objective of this study was to produce taste-masked ibuprofen granules using a novel process, twin-screw melt granulation (TSMG). TSMG is an emerging, high-productivity, continuous process. Granules of ibuprofen embedded in a lipid matrix were produced across a range of process conditions, resulting in a range of output granule particle sizes. The ibuprofen appeared to be miscible with the lipid binder though it recrystallized after processing. The ibuprofen melt granules were tested in simulated saliva using a novel, small-volume dissolution technique with continuous acquisition of the ibuprofen concentration. The ibuprofen release from the granules was slower than the neat API and physical blend, beyond the expected residence time of the granules in the mouth. The ibuprofen release was inversely related to the granule size. A Noyes–Whitney dissolution model was used and the resulting dissolution rate constants correlated well with the granule size.

The Impacts of Crystalline Structure and Different Surface Functional Groups on Drug Release and the Osseointegration Process of Nanostructured TiO2

In implantable materials, surface topography and chemistry are the most important in the effective osseointegration and interaction with drug molecules. Therefore, structural and surface modifications of nanostructured titanium dioxide (TiO2) layers are reported in the present work. In particular, the modification of annealed TiO2 samples with —OH groups and silane derivatives, confirmed by X-ray photoelectron spectroscopy, is shown. Moreover, the ibuprofen release process was studied regarding the desorption-desorption-diffusion (DDD) kinetic model. The results proved that the most significant impact on the release profile is annealing, and further surface modifications did not change its kinetics. Additionally, the cell adhesion and proliferation were examined based on the MTS test and immunofluorescent staining. The obtained data showed that the proposed changes in the surface chemistry enhance the samples’ hydrophilicity. Moreover, improvements in the adhesion and proliferation of the MG-63 cells were observed.

Synthesis and Characterization of Hydrogel of Chitosan-Poly (N-Vinyl-2-Pirrolidone) (PVP)- Alginate for Ibuprofen Release

Hydrogels chitosan-poly-(N-vinyl-pyrrolidone)-alginate (Ch/PVP/Alg) have been synthesized with Ca2+, Zn2+ and formaldehyde as crosslinker. Hydrogels with ratio polymer 70:20:10 give a high swelling ratio and good network. The Ch/PVP/Alg/Ca2+ has 463.73% swelling ratio and 80.59% gel. Ch/PVP/Alg/Zn has 489.21% swelling ratio and 81.67% gel. Ch/PVP/Alg crosslinked with formaldehyde result 488.03% swelling ratio and 85.34% gel. Dissolution test of hydrogels in pH 1.2 releases ibuprofen less than 30%. Whereas in the pH 7.4, the release of ibuprofen by hydrogels are relatively high. Ch/PVP/Alg/Ca reach up to 34.63% in 30 minutes and 40.86% for Ch/PVP/Alg/Zn. Meanwhile Ch/PVP/Alg/CH2O can release 44.92% of ibuprofen in 30 minutes. The obtained hydrogel was characterized using infrared (FTIR) spectrophotometry, differential scanning calorimetry (DSC) and scanning electron microscopy (SEM).

Fabrication of tri-layered electrospun polycaprolactone mats with improved sustained drug release profile

Modulation of initial burst and long term release from electrospun fibrous mats can be achieved by sandwiching the drug loaded mats between hydrophobic layers of fibrous polycaprolactone (PCL). Ibuprofen (IBU) loaded PCL fibrous mats (12% PCL-IBU) were sandwiched between fibrous polycaprolactone layers during the process of electrospinning, by varying the polymer concentrations (10% (w/v), 12% (w/v)) and volume of coat (1 ml, 2 ml) in flanking layers. Consequently, 12% PCL-IBU (without sandwich layer) showed burst release of 66.43% on day 1 and cumulative release (%) of 86.08% at the end of 62 days. Whereas, sandwich groups, especially 12% PCLSW-1 & 2 (sandwich layers—1 ml and 2 ml of 12% PCL) showed controlled initial burst and cumulative (%) release compared to 12% PCL-IBU. Moreover, crystallinity (%) and hydrophobicity of the sandwich models imparted control on ibuprofen release from fibrous mats. Further, assay for cytotoxicity and scanning electron microscopic images of cell seeded mats after 5 days showed the mats were not cytotoxic. Nuclear Magnetic Resonance spectroscopic analysis revealed weak interaction between ibuprofen and PCL in nanofibers which favors the release of ibuprofen. These data imply that concentration and volume of coat in flanking layer imparts tighter control on initial burst and long term release of ibuprofen.

Physicochemical Characterization of Sus scrofa domesticus Fat and a Preliminary Evaluation of its Potential as a Matrix Former in Ibuprofen Granules

Background: There is an increasing interest and search for local and natural sources as active pharmaceutical excipients.Purpose: The study aimed at investigating the physicochemical characteristics of Sus scrofa domesticus (SSD) fat and its potential as a matrix former in ibuprofen granule formulations.Methods: SSD fat was extracted from the domestic pig by wet rendering and purified. The fat was characterized for its organoleptic and physicochemical properties and used in the formulation of batches of ibuprofen granules by melt granulation using varying concentrations (5.0-15%w/w). Conventional granules were formed with maize starch (15%w/w) for control. Formulated granules were evaluated for flow properties, encapsulated in hard gelatin capsules and subjected to in-vitro drug release studies.Results: SSD fat was snow white in colour. Soluble in organic solvents but insoluble in water. pH of the fat was 7.4, viscosity (147.4 millipascal), peroxide value (11.0 meq/kg), acid value (3.4) and saponification value (196.3). Granules formulated with SSD fat exhibited poor flowability and their dissolution profiles showed retardation in ibuprofen release with increase in fat concentrations. Granules formulated with 5.0 and 10%w/w of the fat exhibited 43 and 27% ibuprofen release within 4 h while the conventional granules showed a drug release of 98% within 1.0 h.Conclusion: The physicochemical properties of SSD fat was found to possess favourable potential properties relevant in the formulation of a drug delivery system. The retardation of ibuprofen release from the granules showed that SSD fat has a potential application as a matrix former in controlled release formulation. Keywords: Sus scrofa domesticus, ibuprofen, matrix granules, dissolution profiles