Fabrication and characterization of dexibuprofen nanocrystals using microchannel fluidic rector

Abstract

PurposeDexibuprofen is an enantiomer of ibuprofen with low bioavailability which results from its hydrophobic nature. Nanosuspensions have developed a podium to solve the in vitro dissolution problem that frequently occurs in current research.Materials and methodsThe drug and polymer solutions were mixed in a microchannel fluid reactor and the successive embryonic nanosuspension was decanted into a vial having the polymer solution. The impact of different process and formulation parameters including inlet angle, antisolvent and solvent flow rate(s), mixing time, drug concentration, polymer type and concentration was evaluated.Results and discussionStable dexibuprofen nanocrystals with a particle size of 45±3.0 nm and polydispersity index of 0.19±0.06 were obtained. Differential scanning calorimetry and powder X-ray diffraction confirmed the crystallinity. The key parameters observed were inlet angle 10°, antisolvent to solvent volume of 2.0/0.5 mL/min, 60 minutes mixing with 5 minutes sonication, Poloxamer-407 with a concentration of 0.5% w/v and drug concentration (5 mg/mm). The 60-day stability studies revealed that the nanocrystals were stable at 4°C and 25°C. The scanning electron microscopy and transmission electron microscopy images showed crystalline morphology with a homogeneous distribution.ConclusionStable dexibuprofen nanocrystals with retentive distinctive characteristics and having marked dissolution rate compared to raw and marketed formulations were efficiently fabricated. In future perspectives, these nanocrystals could be converted to solid dosage form and the process can be industrialized by chemical engineering approach.

Solubility and Dissolution Enhancement of Dexibuprofen with Hydroxypropylbetacyclodextrin (HPβCD) and Poloxamers (188/407) Inclusion Complexes: Preparation and In Vitro Characterization

“…PXM-188 had a vast globular shape [46][47][48][49], and PXM-407 also had globular spiral shape, but it does not have as fine a shape as PXM-188 (Figure 4B,C). The SEM images of ternary inclusion complexes showed that the crystallinity was reduced because of ternary inclusion complex formation and uniform drug dispersion within carrier molecules [50].…”

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“…The microchannel fluidic reactor was used with different inlet angles i.e., 10 °, 25 °and 50 °. Various parameters were assessed to figure out newly produced particles i.e., inlet angle, stirring time, solvent-antisolvent flow rates and ultra-sonication (Khan et al, 2018a).…”

“…The samples of raw Indomethacin as well as its nanocrystals were separately added to the aluminum pan and scanned under a nitrogen atmosphere. The samples were scanned between 60 to 190°C at a scanning rate of 10°C/min in triplicate (Khan et al, 2018e).…”