Transdermal nicotine mixed natural rubber-hydroxypropylmethylcellulose film forming systems for smoking cessation:in vitroevaluations

Abstract

Novel film forming polymeric dispersions for transdermal nicotine delivery were prepared from deproteinized natural rubber latex (DNRL) blended with hydroxypropylmethylcellulose (HPMC) and dibutyl phthalate (DBP) or glycerin (GLY) as plasticizer. The preliminary molecular compatibility of ingredients was observed by Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray diffractometry characterizations. All film forming polymeric dispersions were elegant in appearance and smooth in texture without agglomeration. Their pH was 7-8. In addition, their viscosity and spreadability showed good characteristics depended on HPMC and plasticizers blended. The transparent in situ dry films with good strength and elasticity were also confirmed by peeling-off. The nicotine release from them revealed an initial fast release that was similar to the release from a concentrated nicotine solution, and followed by slow release pattern from the in situ films. GLY blended formulation produced a higher amount of nicotine permeation through the in vitro pig skin than DBP blends. Ethanol mixing also enhanced nicotine permeation, but it affected the integrity of in situ films. The nicotine release and skin permeation kinetics were by a diffusion mechanism that was confirmed by the Higuchi's model. These formulations were safe without producing any severe skin irritation. However, for the stability they needed to be stored at 4 °C in tightly sealed containers.

Madecassoside and Asiaticoside-Loaded Film-Forming Polymeric Solutions Based on Hypromellose E5 and Eudragit® NE 30D

“…Moreover, the variation of skin pH between 4.0 -5.96 was reported [31]. The FFPS with a slightly basic pH (approximately 7.6 -9.0) could be found in the other works [13,19]. However, the skin irritation test should be performed to ensure the safety of the FFPS formulation.…”

“…The transparency of the obtained film is an important feature that considerably affects patient compliance [12]. Some drugs can be delivered by this system, i.e., steroid-based drugs such as betamethasone-17-valerate [15] and ethinylestradiol [16], a non-steroidal anti-inflammatory drug such as ketorolac [17], an antifungal agent such as naftifine hydrochloride [18], and drug for smoking cessation such as nicotine [13,19]. Besides, plant extract, the α-mangostin is incorporated into FFPS for antibacterial application [20].…”

“…Several polymers are introduced to use as a film-forming agent such as Eudragit ® Trends Sci. 2022; 19(21): 796 2 of 10 [ [14][15][16][21][22][23], hypromellose [19,20], deproteinized natural rubber latex [13,19], polyvinyl alcohol [13,24], etc. Hypromellose is widely used in oral, ophthalmic, nasal, and topical formulations [25].…”

Solvent‐Cast Polymeric Films from Pectin and Eudragit® NE 30D for Transdermal Drug Delivery Systems

“…They are used as packaging materials, tablet coatings to protect drugs from environmental factors, and matrix layers to control the release of the drug, among others. Polymer lms are also used in the preparation of transdermal formulations for delivering drugs to the skin, e.g., polymethylmethacrylate for lidocaine hydrochloride (1), ethyl cellulose blended with deproteinized natural rubber latex for ketoprofen patches (2), deproteinized natural rubber latex-based polymer blends (3)(4)(5)(6) and pectin-based polymer blends for nicotine patches (7)(8)(9), chitosan-based polymer blends for Thai herbal patches (10,11), and polydimethylsiloxane and ethylcellulose for centchroman patches (12). These polymeric matrix drug-containing lms can be used in treatment where drug release must be controlled and provide increased drug concentrations through the skin into the blood.…”