Development and evaluation of buccal films impregnated with selegiline-loaded nanospheres

Abstract

Poor peroral therapeutic efficiency of selegiline is primarily due to the extensive hepatic metabolism and hence the need for an alternative route of administration. The present study is based on evaluation of a buccal film which is impregnated with selegiline nanospheres to enhance the systemic bioavailability. Selegiline-loaded nanospheres prepared using poly(lactide-co-glycolide) was embedded into buccal films (F 1 -F 4 ) with varying polymer composition [hydroxypropyl methylcellulose and eudragit]. The developed films were evaluated for their physicomechanical properties, hydration, mucoadhesive strength, in vitro drug release and ex vivo permeation in order to identify the ideal system suitable for further development. In vivo studies were carried out on rabbits to assess the comparative pharmacokinetics profile of the selected buccal film with oral solution. Preliminary studies indicated that the prepared films exhibited excellent physical properties, adequate mucoadhesive strength and moderate hydration. In vitro drug release data of the buccal films (F 1 , F 2 and F 3 ) showed distinct profiles. Permeation studies indicated higher steady-state flux from film F 3 (p50.0001) when compared to film F 2 . In-vivo results of film (F 3 ) demonstrated significant increase in absorption (p50.0001), C max ($1.6-fold), T max , AUC 0-a ($3-fold, p50.0001) and improved bioavailability, when compared to control. This study concludes that the buccal delivery of selegiline using the developed buccal film (F 3 ) would be a promising alternative approach for the treatment of Parkinson's disease.

HPMC- and PLGA-Based Nanoparticles for the Mucoadhesive Delivery of Sitagliptin: Optimization and In Vivo Evaluation in Rats

“…A mucoadhesive drug delivery system provides various advantages by targeting and localizing the nanoparticles at a target site, by decreasing variation in drug level in the plasma, and by extending residence time at the confined target site of drug penetration, and thereby reducing side effects [5][6][7]. Nanoparticles offer promising drug delivery technology by improving the therapeutic window and increasing their tolerability and enhancing their efficacy in the body.…”

In vitro and in vivo evaluation of nano-based films for buccal delivery of zolpidem

“…Previous studies have shown the combination of carbopol 974P and HPMC K100 provides adequate swelling and mucoadhesive strength to the film. 15,18,26 Different combinations of these three polymers were mixed to form films of varying composition (named Z1-Z4). Previous literature notes that these polymers are capable of controlling the release of pharmaceutically active compounds.…”

“…The solution was then centrifuged at 10,000 rpm for 2 min, then the supernatant was filtered and analyzed by HPLC. 15 …”

Development of Asialoglycoprotein Receptor-Targeted Nanoparticles for Selective Delivery of Gemcitabine to Hepatocellular Carcinoma

“…The EE of drug is mainly dictated by the partition coefficient of the drug and its inherent solubility in the specific polymer. However, the solubility of drug in polymer is normally influenced by the physicochemical properties (molecular weight and chemical nature of drug and polymer) as well as the probable drug-polymer interaction [31]. The effect of polymer concentration (40-200 mg) on the %EE and %DL values were assessed and are depicted in Table 1.…”