Preparation of Ibuprofen Microparticles by Antisolvent Precipitation Crystallization Technique: Characterization, Formulation, and In Vitro Performance

Abstract

This study demonstrates the preparation and characterization of ibuprofen (IBP) microparticles with some excipients by a controlled crystallization technique with improved dissolution performance. Using the optimum concentrations pluronic F127, hydroxypropyl methyl cellulose, D-mannitol, and l-leucine in aqueous ethanol, the IBP microparticles were prepared. The dissolution tests were performed in phosphate buffer saline using a United States Pharmacopoeia dissolution tester at 37°C. The Raman spectroscopy was used to investigate the interactions and distribution of the IBP with the additives in the microcrystals. The prepared IBP microparticles showed higher dissolution compared to that of the smaller sized original IBP particles. The Raman data revealed that the excipients with a large number of hydroxyl groups distributed around the IBP particle in the crystal enhanced the dissolution of the drug by increasing the drug-solvent interaction presumably through hydrogen bonding. The Raman mapping technique gave an insight into the enhanced dissolution behavior of the prepared IBP microparticles, and such information will be useful for developing pharmaceutical formulations of hydrophobic drugs. The controlled crystallization was a useful technique to prepare complex crystals of IBP microparticles along with other additives to achieve the enhanced dissolution profile.

Tailoring of Solubility of Ibuprofen in the Presence of Hydrophilic Excipients in Water-Ethanol Mixtures by Crystallization Method

“…S2). Very recently, the hydrophilic Pl F127 found to closely associate with Ibu particle and strongly promoted Ibu wettability by reducing the surface tension [14]. Thus, the outcome of this study suggests that Pl F127 caused to increase the Ibu solubility linearly with its concentration in water and aqueous ethanol solvents.…”

“…The main purpose of using polymeric stabilizers was to ensure the stability of Ibu nanosuspensions on a short term storage and to achieve successful formation of nanocrystals during particle production and both the HPMC and the Pl F127 serve these purposes effectively [10,11,13,14]. In this study, the effect of the combined excipients on the Ibu solubility were investigated at three levels of aqueous ethanol (0, 10, 20% w/w, E/(E+W)) and the concentration of the excipients was varied up to 2%, w/w as [Pl F127+HPMC)/[E+W).…”

“…Khan determined the Ibu solubility in ethanol and aqueous solution of HPMC and Pl F127 at four temperatures (15,25,35 and 45 °C) for controlled precipitation crystallization [13]. Recently, Afrina et al prepared and characterized the Ibu microparticles with some excipients (Pluronic F127, HPMC, D-mannitol and L-leucine) by a controlled crystallization technique with improved dissolution performance [14]. In current study, we explored the effect of some pharmaceutical excipients such as HPMC, Pl F127, mannitol and leucine on Ibu solubility in water ethanol co-solvents.…”

Puerarin dry powder inhaler formulations for pulmonary delivery: Development and characterization

“…The Raman mapping was done for formulation F3 with lactose, Mg-St and puerarin. In Fig 6 , image A is a combination of all the components and illustrates that all are uniformly distributed in the mixture and puerarin particles are adhered on the surface of the lactose particles with Mg-St surrounding it which is expected to help the particle flow freely and detach from the carrier surfaces during inhalation [ 35 ]. Other images represent the individual components of the mixture as (B) representing Puerarin, (C) lactose, and (D) MgSt.…”

Excipient Interactions in Glucagon Dry Powder Inhaler Formulation for Pulmonary Delivery

“…Raman microscopy, a non-destructive analytical technique, has previously been used to visualize the component distribution of powder mixtures [19]. Very recently, Afrina et al demonstrated the application of Raman spectroscopy to investigate the interactions and distribution of ibuprofen crystallized with other additives [20]. Fourier-transform infrared spectroscopy (FTIR) was used to study the interactions of powders (drug and excipients) in interactive mixtures [21,22].…”