advertisement
Abstract #27296 Published in IGR 12-4
Improved ocular absorption kinetics of timolol maleate loaded into a bioadhesive niosomal delivery system
Kaur IP; Aggarwal D; Singh H; Kakkar SGraefe's Archive for Clinical and Experimental Ophthalmology 2010; 248: 1467-1472
Background: Application of timolol maleate (TM) in a conventional dosage form (solution) into the eye results in almost 80% of the instilled dose being lost either through spillage or due to drainage into the nasolacrimal duct. Later results in systemic side-effects especially in patients suffering from heart diseases or bronchial asthma thus limiting the usefulness of TM for the control of glaucoma. Earlier we had reported on the development of a mucoadhesive coated niosomal system for TM (TM REV(bio)) containing 0.25% TM. Presently we establish and report the pharmacokinetic and pharmacodynamic superiority of the developed ocular formulation of TM. Methods: Aqueous humor concentration of TM in male albino rabbits, after instillation of one drop of TM solution (TMS) or TMREV(bio) was measured using the microdialysis method. Results: Peak concentration of drug in aqueous humor from TMREV(bio) (12.46 (mu)g/ml achieved at 60 min) was almost 1.7 times that of the control drug solution (TMS, 0.25%; 7.2 (mu)g/ml). An important observation was that the high drug concentrations achieved upon TMREV (bio) administration were maintained for up to 2 h. AUC for TMREV (bio) formulation was 2.34 times that of the TMS. Conclusions: This study confirms a sustained and controlled effect of the developed formulation. (copyright) 2010 Springer-Verlag.
I. P. Kaur. University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India. indupalkaur@yahoo.com
Classification:
11.16 Vehicles, delivery systems, pharmacokinetics, formulation (Part of: 11 Medical treatment)
11.3.4 Betablocker (Part of: 11 Medical treatment > 11.3 Adrenergic drugs)
