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Published on: March 9, 2019
Formulation, Development, and In vitro Evaluation of Sustained Release Buccal Films for Optimized Memantine Therapy.
Dushyant1, Subhashish Nayak1, Vrint Panchal1
1Global Research Institute of Pharmacy, Radaur, 135133, Yamuna Nagar, Haryana, India.
New sustained-release buccal films of memantine hydrochloride offer a promising alternative for Alzheimer's disease treatment. These films enhance drug delivery, potentially improving patient compliance and systemic availability by bypassing first-pass metabolism.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Biomaterials
Background:
- Memantine, an N-methyl-D-aspartate (NMDA) receptor antagonist, is used for moderate to severe Alzheimer's disease.
- Oral memantine exhibits low bioavailability due to first-pass metabolism, necessitating frequent dosing.
- Buccal drug delivery presents an alternative to improve systemic availability and patient compliance.
Purpose of the Study:
- To develop and characterize sustained-release buccal films of memantine hydrochloride.
- To evaluate the potential of buccal films as a noninvasive alternative drug delivery system for memantine.
Main Methods:
- Sustained-release buccal films were prepared using Hydroxypropyl Methylcellulose (HPMC) and Carbopol 940 via solvent casting.
- Polyethylene glycol 400 and menthol were used as plasticizer and permeation enhancer, respectively.
- Films were analyzed for physicochemical properties, mechanical strength, swelling, surface pH, drug content, residence time, and in vitro drug release.
Main Results:
- Prepared films exhibited uniform thickness, good mechanical properties, and buccal mucosa-compatible surface pH.
- Films demonstrated sustained drug release for 8 hours with no chemical incompatibility between memantine and excipients.
- Optimized film (F11) showed high drug content (90.1%), good swelling index (19.4%), and a residence time of approximately 5 hours.
Conclusions:
- Developed memantine hydrochloride buccal films possess favorable physicochemical and in vitro release properties.
- The films show potential as a noninvasive alternative drug delivery system, improving systemic availability and patient compliance.
- Further in vivo and ex vivo studies are required to confirm the pharmacokinetic benefits of this buccal delivery system.
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