Nifedipine nanoparticle agglomeration as a dry powder aerosol formulation strategy.
Efficient administration of drugs represents a leading challenge in pulmonary medicine. Dry powder aerosols are of great interest compared to traditional aerosolized liquid formulations in that they may offer improved stability, ease of administration, and simple device design. Particles 1-5microm in size typically facilitate lung deposition. Nanoparticles may be exhaled as a result of their small size; however, they are desired to enhance the dissolution rate of poorly soluble drugs. Nanoparticles of the hypertension drug nifedipine were co-precipitated with stearic acid to form a colloid exhibiting negative surface charge. Nifedipine nanoparticle colloids were destabilized by using sodium chloride to disrupt the electrostatic repulsion between particles as a means to achieve the agglomerated nanoparticles of a controlled size. The aerodynamic performance of agglomerated nanoparticles was determined by cascade impaction. The powders were found to be well suited for pulmonary delivery. In addition, nanoparticle agglomerates revealed enhanced dissolution of the drug species suggesting the value of this formulation approach for poorly water-soluble pulmonary medicines. Ultimately, nifedipine powders are envisioned as an approach to treat pulmonary hypertension.
Plumley
Carl
C
Department of Chemical and Petroleum Engineering, The University of Kansas, Lawrence, KS 66047, United States of America.
Gorman
Eric M
EM
El-Gendy
Nashwa
N
Bybee
Connor R
CR
Munson
Eric J
EJ
Berkland
Cory
C
D000336:Aerosols; D002121:Calcium Channel Blockers / Q000008:administration & dosage* / Q000493:pharmacokinetics; D003102:Colloids; D016503:Drug Delivery Systems; D004355:Drug Stability; D006976:Hypertension, Pulmonary / Q000188:drug therapy; D053758:Nanoparticles; D009543:Nifedipine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D010316:Particle Size; D011208:Powders; D012965:Sodium Chloride / Q000737:chemistry; D012995:Solubility; D055672:Static Electricity; D013229:Stearic Acids / Q000737:chemistry; D014018:Tissue Distribution
D000336:Aerosols; D002121:Calcium Channel Blockers; D003102:Colloids; D011208:Powders; D013229:Stearic Acids; D012965:Sodium Chloride; C031183:stearic acid; D009543:Nifedipine