Solubility and dissolution rate enhancement of ibuprofen by cyclodextrin based carbonate nanosponges.

Shoaib, Qurat-ul-ain; Latif, Sumera; Ijaz, Qazi Amir; Afzal, Hafsa; Siddique, Muhammad Irfan; Hussain, Amjad; Arshad, Muhammad Sohail; Bukhari, Nadeem Irfan; Abbas, Nasir

In the present study nanotechnology approach, i.e., a cyclodextrin (CD) based carbonate nanosponge was used to improve the solubility and dissolution of ibuprofen. Solvent and ultrasound assisted methods were used to prepare nanosponges using two CDs (β-CD and 2-hydroxypropyl-β-CD (2HP-β-CD)) and a cross-linker (CL) diphenyl carbonate (DPC) in varying molar ratios. Nanosponges were investigated for their solubilizing efficiency and phase solubility studies. Structural analysis by Fourier transform infrared (FTIR) and powder X-ray diffraction (PXRD), thermoanalytical characterization by differential scanning calorimetry (DCS), morphology by scanning electron microscopy (SEM). In-vitro drug release followed by in-vivo analgesic and anti-inflammatory studies were performed. 2HP-β-CD based nanosponges (molar ratio 0.01:0.04) prepared by ultrasound assisted method showed the highest solubilizing efficiency (i.e., 4.28 folds). Stability constant values showed that all complexes were stable. Inclusion complexes of drug was confirmed by PXRD and DSC. SEM images showed porous structures confirming the formation of cross-linked network. Particle size was in the range of 296.8±64 to 611.7±32nm. In-vitro release studies showed enhanced dissolution profile from nanosponge formulation (~94% from I11) as compared to the pure drug (~45% Ibuprofen) in 120min. Significant (p<0.05) extent of pain inhibition and anti-inflammatory activity was observed for nanosponge formulation when compared with the pure drug. CD based carbonate nanosponges with better solubility, enhanced release profile, improved analgesic and anti-inflammatory activity were successfully formulated for ibuprofen.

IBUPROFEN; SOLUBILITY; STABILITY constants; X-ray powder diffraction; DIFFERENTIAL scanning calorimetry

Pakistan Journal of Pharmaceutical Sciences, 2021, Vol 34, p1045

1011-601X

Academic Journal

10.36721/PJPS.2021.34.3.SUP.1045-1055.1