Abstract
Nimodipine (NMD) is a dihydropyridine calcium channel blocker useful for the prevention and treatment of delayed ischemic effects. It belongs to class ? drugs, which is characterized by low solubility and high permeability. This research aimed to prepare Nimodipine nanoparticles (NMD NPs) for the enhancement of solubility and dissolution rate. The formulation of nanoparticles was done by the solvent anti-solvent technique using either magnetic stirrer or bath sonicator for maintaining the motion of the antisolvent phase. Five different stabilizers were used to prepare NMD NPs( TPGS, Soluplus®, HPMC E5, PVP K90, and poloxamer 407). The selected formula F2, in which Soluplus 
 has been utilized as a stabilizer, has a particle size (77 nm) and polydispersity index (PDI) (0.016). The formulas with the smallest particle size were freeze dried with the addition of 1 % w/w mannitol as cryoprotectant. The saturation solubility of NMD in the prepared nanoparticles was increased twenty four-folds, and the complete dissolution was achieved at 90 minutes compared with pure NMD, which reaches only 6%. The formation of hydrogen bonding between NMD and the polymer or the cryoprotectant, as confirmed by the FTIR study. In conclusion, the preparation of NMD as polymeric nanoparticles is a useful technique for enhancing the solubility and dissolution rate.
Highlights
Many new pharmaceutical entities, approximately 40 % of them, are lipophilic compounds which have low water solubility and raise a clinical issue regarding their dissolution and absorption from their administration sites[1].The solubility of drugs in aqueous media is an essential consideration to be dealt with early in the drug discovery process, and several formulation strategies have been proposed to enhance the solubility, such as complexation, pH adjustment, and using co-solvents[2].Nanoparticles (NPs) are solid colloidal particles that usually lie in the 100 nm size range[3]
All the samples of NMD NS were analyzed by the ABT-9000 nanolaser particle size analyzer, and the particle size distribution of all formulas was recorded, as shown in table [2]
polydispersity index (PDI) is an essential means to evaluate the particle size distribution within the sample. It is crucial in determining the uniformity of particle size, which is valuable in the stability of a nanosuspension
Summary
Approximately 40 % of them, are lipophilic compounds which have low water solubility and raise a clinical issue regarding their dissolution and absorption from their administration sites[1].The solubility of drugs in aqueous media is an essential consideration to be dealt with early in the drug discovery process , and several formulation strategies have been proposed to enhance the solubility, such as complexation, pH adjustment, and using co-solvents[2].Nanoparticles (NPs) are solid colloidal particles that usually lie in the 100 nm size range[3]. This method involves dissolving 30 mg of NMD in 3 ml ethanol ( solvent ) and allowed to be added dropwise using syringe pump as shown in figure(2 ) at a speed of 1 ml/min into a beaker containing 27 ml distilled water (antisolvent in presence of (60 mg) of the following stabilizers ( TPGS, Soluplus, HPMC E5, PVP K90, poloxamer 407) and this process was done using either magnetic stirrer at a speed of 300 rpm or bath sonicator[17].
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Schedule a callMore From: Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)
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