Impact of in situ granulation and temperature quenching on crystal habit and micromeritic properties of ibuprofen-cationic dextran conjugate crystanules

Thermodynamic Changes Induced by Intermolecular Interaction Between Ibuprofen and Chitosan: Effect on Crystal Habit, Solubility and In Vitro Release Kinetics of Ibuprofen

“…Pure ibuprofen (Fig. 2a) exhibits distinct rod-like shape with smooth regular surface and average size 453.88 ± 29.8469 × 97.12 ± 5.4267 μm (aspect ratio 5.16±1.15) as reported previously (4). Chitosan showed rough surface and irregular polyhedral shapes.…”

“…Also, the melting point of ibuprofen decreased remarkably with chitosan concentration, from 80.07±1.76 to 56.90± 0.88°C (p<0.05; n=6) at 26.24×10 −3 g/dm 3 chitosan, corresponding to 28.94% decrease in crystallinity of ibuprofen. We have reported similar binary amorphous ibuprofen-Ddex conjugate crystanules prepared by melt-in situ granulation-crystallizaton technique(4). The TGA curves of pure ibuprofen and the IB-CT nanoplex FT-IR spectra of (a) pure ibuprofen; (b) chitosan powder; IB-CT nanoplex containing (c) 0.82; (d) 1.64 (e) 3.28; (f) 6.56; (g) 13.12 and (h) 26.24×10 −3 g/dm 3 CT respectively.…”

“…However because of its needle-like (acicular) crystalline nature, viscoelastic and high cohesive characteristics, low solubility (49 μg/ml at 25°C) and short biological half-life (2 h), ibuprofen has been difficult to formulate and when administered orally, large and multiple doses are usually required, leading to wasted dosing and potentially serious side effects such as ulceration and bleeding (4,5,13). Therefore there is continuous research interest to enhance the biopharmaceutical properties and system specific parameters of ibuprofen.…”

Polymer-Drug Nanoconjugate – An Innovative Nanomedicine: Challenges and Recent Advancements in Rational Formulation Design for Effective Delivery of Poorly Soluble Drugs

“…This hypothesis corresponds with our findings in ibuprofen-Ddex conjugates where ibuprofen molecule was internalized into the Ddex shell structure (Fig. 8C, 8D) (159). In order to optimize characterization of polymer-drug nanoconjugates and enhance the opportunity of successful translation into clinically useful nanomedicines, future trend of characterization techniques should include molecular recognition of the polymer matrix at specific receptor at the cellular level including the specific drug targeting ligands.…”

“…The more pronounced effects of cationic conjugates has been attributed to the presence of a high load of negatively charged sialic acid residues on cancer cell surface facilitating effective cationic conjugate absorption. In our laboratory we have investigated the impact of cationic diethylaminoethyl dextran (Ddex) on crystal behaviour and micromeritics properties of ibuprofen in ibuprofenDdex conjugate crystanules (159). We have also investigated the direct effect of ibuprofen-Ddex interaction on the solubility, dose distribution, dissolution velocity, pre-compression and compression charactistics of ibuprofen (160,161).…”