Biodegradable PLGA microspheres loaded with ganciclovir for intraocular administration. Encapsulation technique, in...

Area of Science:

• Ophthalmology
• Materials Science
• Drug Delivery

Background:

• Intraocular drug delivery faces challenges with frequent administration and systemic side effects.
• Sustained-release formulations are crucial for improving therapeutic efficacy and patient compliance.
• Biodegradable polymers like PLGA offer potential for controlled drug release applications.

Purpose of the Study:

• To develop a sterilized formulation of poly (DL-lactide-co-glycolide) (PLGA) microspheres for sustained intraocular delivery of ganciclovir.
• To evaluate the impact of gamma radiation sterilization on the physicochemical properties and drug release profile of ganciclovir-loaded PLGA microspheres.

Main Methods:

• Microspheres were prepared using a drug-in-oil dispersion method with PLGA in acetone and ganciclovir in fluorosilicone oil.
• Formulations were emulsified, collected, and sterilized using gamma radiation (2.5 megarads).
• In vitro drug release studies and comparison between sterilized and non-sterilized batches were conducted using the similarity factor (f2).

Main Results:

• High drug loading efficiency of up to 95% was achieved in microspheres (300-500 microm).
• In vitro release demonstrated sustained ganciclovir release over 42 days, with an initial burst followed by a slower release rate.
• No significant differences in drug encapsulation or dissolution profiles were observed between sterilized and non-sterilized microspheres.

Conclusions:

• The developed PLGA microsphere formulation enables high ganciclovir loading and sustained intraocular drug release.
• Gamma radiation sterilization is a viable method for this formulation, maintaining drug integrity and release characteristics.
• This approach holds promise for effective intraocular treatment of viral infections.