Nanosuspension as an ophthalmic delivery system for certain glucocorticoid drugs.
Poorly-water-soluble compounds are difficult to develop as drug products using conventional formulation techniques. The use of nanotechnology to formulate poorly-water-soluble drugs as nanosuspensions offers the opportunity to address many of the deficiencies associated with this class of molecules. In the present study, the high pressure homogenization method used to prepare nanosuspensions of three practically insoluble glucocorticoid drugs; hydrocortisone, prednisolone and dexamethasone. The effect of particle size in the micron and nano-size ranges as well as the effect of viscosity of the nanosuspension on the ocular bioavailability was studied by measuring the intraocular pressure of normotensive Albino rabbits using shiØetz tonometer. The results show that compared to solution and micro-crystalline suspensions it is a common feature of the three drugs that the nanosuspensions always enhance the rate and extent of ophthalmic drug absorption as well as the intensity of drug action. In the majority of cases nanosuspensions extend the duration of drug effect to a significant extent. The data presented confirms that nanosuspensions differ from micro-crystalline suspensions and solution as ophthalmic drug delivery systems and that the differences are statistically, highly to very highly significant. The results confirm also the importance of viscosity of nanosuspension especially in increasing the duration of drug action.
Kassem
M A
MA
Department of Pharmaceutical Technology, National Research Center, Dokki, Cairo, Egypt.
Abdel Rahman
A A
AA
Ghorab
M M
MM
Ahmed
M B
MB
Khalil
R M
RM
D000287:Administration, Topical; D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D003907:Dexamethasone / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D004337:Drug Carriers; D004339:Drug Compounding; D005123:Eye / Q000378:metabolism*; D005938:Glucocorticoids / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D006854:Hydrocortisone / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D007429:Intraocular Pressure / Q000187:drug effects; D008297:Male; D053758:Nanoparticles; D009883:Ophthalmic Solutions; D010316:Particle Size; D011239:Prednisolone / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D011312:Pressure; D011817:Rabbits; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods; D014783:Viscosity; D014867:Water / Q000737:chemistry
D004337:Drug Carriers; D005938:Glucocorticoids; D009883:Ophthalmic Solutions; D014867:Water; D003907:Dexamethasone; D011239:Prednisolone; D006854:Hydrocortisone