ABSTRACT
Niosomes are nonionic surfactant vesicles that have potential applications in the delivery of hydrophobic and hydrophilic drugs. Permeation of a potent nonsteroidal anti-inflammatory, ketorolac, across excised rabbit skin from various proniosome gel formulations was investigated using Franz diffusion cells. Each of the prepared proniosomes significantly improved drug permeation and reduced the lag time (P<0.05). Proniosomes prepared with Span 60 provided a higher ketorolac flux across the skin than did those prepared with Tween 20 (7- and 4-fold the control, respectively). A change in the cholesterol content did not affect the efficiency of the proniosomes, and the reduction in the lecithin content did not significantly decrease the flux (P>0.05). The encapsulation efficiency and size of niosomal vesicles formed by proniosome hydration were also characterized by specific high performance liquid chromatography method and scanning electron microscopy. Each of the prepared niosomes achieved about 99% drug encapsulation. Vesicle size was markedly dependent on the composition of the proniosomal formulations. Proniosomes may be a promising carrier for ketorolac and other drugs, especially due to their simple production and facile up.
Subject(s)
Drug Carriers/administration & dosage , Drug Delivery Systems/methods , Ketorolac/administration & dosage , Administration, Cutaneous , Animals , Chemistry, Pharmaceutical , Drug Carriers/chemical synthesis , Drug Carriers/pharmacokinetics , Drug Compounding , Ketorolac/pharmacokinetics , RabbitsABSTRACT
Isoniazid (INH) albumin microspheres were prepared by two different stabilization processes: chemical denaturation using glutaraldehyde and heat denaturation. The extent of stabilization was characterized by the solubility of the microspheres. In vitro drug release rates were correlated to the stability of the microspheres and the results showed that the more denatured the albumin by heat stabilization, the slower the drug release rate. A factorial concept has been utilized to synthesize microspheres suitable for passive targeting to the lungs by varying protein concentration, stabilization temperature, time and aqueous volume. These factors significantly affected the sphere size, payload and a release profile of the drug. As the severity of the denaturation conditions increased, the payload decreased and the rate of drug release was slowed. The microspheres carrying isoniazid were followed in experimental animals to validate the targeting process.
