Abstract
Objective: The present research work aims to develop an abuse deterrent rapidly dissolving buprenorphine microemulsion loaded sublingual film for the treatment of breakthrough pain.
 Methods: The Buprenorphine microemulsion loaded sublingual films were prepared using Capmul MCM C8 (oil), tween 20 (surfactant) and propylene glycol (co-surfactant) with different grades of film-forming polymer (HPMC) using film casting machine. The films were evaluated for in vitro disintegration and dissolution study, tensile strength, folding endurance, content uniformity, surface pH, thickness and weight variation, % loading of buprenorphine microemulsion in sublingual film, scanning electron microscope, ex vivo permeation study, droplet size and polydispersity index, Zeta potential, % moisture content, stability and abuse deterrent potential were evaluated.
 Results: The optimized film formulation showed desired mechanical properties with minimum disintegration time of 21s and exhibited 34.45 % loading of Buprenorphine microemulsion. Permeation studies through goat sublingual mucosa, indicated 87% Buprenorphine release, through Buprenorphine microemulsion loaded sublingual film, whereas only 30% Buprenorphine release when it was directly added to film without microemulsion strategy.
 Conclusion: The present study concludes that abuse deterrent and fast acting buprenorphine microemulsion-incorporated sublingual film of buprenorphine HCL and naloxone HCL is a promising alternative to mostly marketed buprenorphine injectable delivery systems and a non-invasive route of administration for breakthrough pain management.
Highlights
Buprenorphine hydrochloride (BU) is a partial agonist at mu (μ) and kappa (K) opioid receptor and antagonist at delta receptors used for the treatment of moderate to severe pain as well as chronic pain [1]
In the present study BU microemulsion was incorporated into the sublingual film and for that BU C2 ME with Smix ratio of 1:1 and BU A2 ME with Smix ratio of 2:1 was selected and quantities of each ME was fixed as per solubility, to incorporate 2.16 mg dose of BU
In each of the trial batch the concentration of HPMC E15 was increased in order to obtain the complete incorporation of microemulsion into the sublingual film
Summary
Buprenorphine hydrochloride (BU) is a partial agonist at mu (μ) and kappa (K) opioid receptor and antagonist at delta receptors used for the treatment of moderate to severe pain as well as chronic pain [1]. With respect to buccal formulations, buprenorphine’s buccal film Bunavail®is available in the market. This bilayered film increases the total bioavailability of BU to more than 40% in healthy subjects [6]. Bai et al, carried out the pharmacokinetic study of BU buccal film formulation in healthy volunteers and the study revealed that bioavailability of BU was about 46 to 51% [7]. This indicates further research in the enhancement of the BU is to be carried out for better bioavailability
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
