Development of Polyvinyl Alcohol/Polyethylene Glycol Copolymer-based Orodispersible Films Loaded with Entecavir:...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Entecavir (ETV) is a key antiviral medication for chronic hepatitis B.
• Conventional ETV tablets may present challenges in administration for certain patient populations.
• Orodispersible films (ODFs) offer an alternative dosage form with potential for improved patient compliance.

Purpose of the Study:

• To prepare and characterize entecavir (ETV)-loaded orodispersible films (ODFs).
• To evaluate the dissolution rate, mechanical, and physicochemical properties of the developed ETV-ODFs.
• To assess the stability and drug-excipient compatibility of the ODF formulation.

Main Methods:

• Solvent casting method was employed for ODF preparation.
• Optimization of film-forming agent (Kollicoat® IR), plasticizer, and disintegrating agent.
• Drug-excipient compatibility studies under accelerated conditions (heat, humidity, light).
• Dissolution studies in various pH media, mechanical property testing (tensile strength, elastic modulus, elongation), and physicochemical characterization (SEM, XRD, DSC, FT-IR).

Main Results:

• Optimal ETV-ODF formulation exhibited excellent physical properties, including a disintegration time of 25.31±1.95 s and good mechanical strength.
• Over 90% drug release was achieved within 10 minutes in all tested media.
• The ODFs demonstrated good stability with minimal related substances (<0.5%) after 10 days of accelerated storage.
• SEM, XRD, DSC, and FT-IR confirmed drug dispersibility and potential drug-excipient interactions.

Conclusions:

• The developed entecavir-loaded orodispersible films possess favorable disintegration and dissolution profiles.
• The ODFs exhibit robust mechanical properties suitable for pharmaceutical applications.
• This novel ODF formulation represents a promising alternative to conventional entecavir tablets for chronic hepatitis B treatment.