Title:Propranolol as a Model Drug to Treat Smoking Cessation and its Formulation
as a Transdermal Patch for Effective Management
Volume: 20
Issue: 9
Author(s): Prasanta Kumar Mohapatra*, Rajnish Srivastava, Krishna Kumar Varshney and Sarvasudhi Durga Bhavani
Affiliation:
- Moradabad Educational Trust Group of Institutions, Faculty of Pharmacy, Moradabad, Uttar Pradesh, India
Keywords:
Propranolol, Smoking, Nicotine replacement therapy (NRT), Psychological, polymer, Molecular, Transdermal drug delivery system.
Abstract:
Background: Smoking causes cancer, heart attacks, and stroke and leads to asthma and breathing
problems. Nicotine replacement therapy (NRT) is considered one of the most widely accepted methods
to quit smoking. However, it can lead to relapsed physical and psychological dependence.
Aim: The present study aimed to explore propranolol, as a model drug to treat relapsed physical and psychological
dependence due to NRT in smoking cessation. Furthermore, for its effective management, the
transdermal drug delivery system has opted for the effective and long-term release of propranolol.
Objective: The objective of the present study was to investigate and establish the molecular associations
between propranolol with different targets associated with smoking cessation.
Materials and Methods: The molecular association of propranolol with eight different potential targets,
namely, Acetylcholine Binding Protein (AChBP), Cannabinoid Receptor, CB1 and CB2, Monoamine
oxidase (MAO), human dopamine D3 receptor, kainite, Leu- biogenic amine transporters (BAT) and α-
type peroxisome proliferator-activated receptor, was studied via molecular simulation models. Polymeric
films containing propranolol HCI were prepared and evaluated to select a suitable formulation for
developing transdermal drug delivery systems (TDDS). Films containing different ratios of HPMC K4M,
HPMC 15M, and Sodium CMC were prepared by the solvent evaporation technique using PEG 4000
incorporated as a plasticizer, and SLS was used to act as a penetration enhancer. Manufactured transdermal
films were physically evaluated for thickness, weight uniformity %, moisture content %, moisture
uptake %, drug content % and folding endurance.
Results: Results indicated that propranolol can interact with all eight receptors at the active binding site.
It was found to show considerable interaction with Acetylcholine Binding Protein (AChBP), MAO, human
dopamine D3 receptor, kainite, and Leu- biogenic amine transporters (BAT) with the binding energy
of -6.27, -6.74, -7.07, -6.84, and -6.63 kcal/mol, respectively. The release rate of propranolol HCI
decreased linearly with increasing polymer concentration in the film and depended on the film thickness.
In contrast, the quantity of drug release was proportional to the square root of time. Kinetic data based on
the release exponent, ‘n’ in the Peppas model showed that n values were between 0.95 and 1.08,
indicating that drug release from polymer matrix was predominantly by diffusion with swelling.
Conclusion: Transdermal drug delivery of propranolol could act as a potential regulator of all studied
targets associated with physical and psychological dependence associated with NRT and smoking cessation.
Furthermore, propranolol-loaded transdermal patches with optimized release could be utilized to
deliver the drug with optimum bioavailability for a considerable time.
