Published in Issue 2019-05-08
How to Cite
Jafri, I., Shoaib, M. H., Yousuf, R. I., & Ali, F. R. (2019). Effect of permeation enhancers on in vitro release and transdermal delivery of lamotrigine from Eudragit®RS100 polymer matrix-type drug in adhesive patches. Progress in Biomaterials, 8(2 (June 2019). https://doi.org/10.1007/s40204-019-0114-9
Abstract
Abstract The drug-in-adhesive (DIA)-type matrix patches of lamotrigine are developed using variable permeation enhancers (oleic acid, PG, lemon oil and aloe vera), and drug in vitro release and its permeation are evaluated. Lamotrigine has been long used as an anti-epileptic, mood stabilizer, to treat bipolar disorder in adults and off label as an antidepressant. lamotrigine matrix patches comprising of Eudragit ® RS100 (rate-controlling polymer) and DuroTak ® 387-2510 (adhesive) were prepared by pouring the solution on backing membrane (3M-9720). The thickness of 120 µm was adjusted through micrometer film applicator. USP Apparatus V was used for the evaluation of release profile, which was fitted into various mathematical models. Quality characteristics of patches were determined through weight variation, moisture content, moisture uptake and drug content evaluation. FTIR studies were performed for drug-excipient compatibility; Franz diffusion cell was employed for studying in vitro permeation parameters such as flux, lag time, and ER. Skin sensitivity study of optimized patch was also performed. The release from patches comprising of PG and oleic acid was maximum, i.e., 96.24 ± 1.15% and 91.12 ± 1.11%, respectively. Formulations (A1–A5) exhibited Makoid–Banakar release profile. Formulation A3 consisting of oleic acid was optimized due to enhanced permeation of drug across skin compared to other enhancers with enhancement ratio of 3.55. Skin sensitivity study revealed patch as safe and non-allergenic. The study demonstrates that oleic acid can be used as a suitable permeation enhancer for transdermal delivery of lamotrigine from matrix-type patches.Keywords
- Lamotrigine,
- Transdermal,
- Permeation enhancer,
- Oleic acid,
- Propylene glycol,
- Eudragit®RS100
References
- Aggarwal et al. (2013) Formulation, in vitro and in vivo evaluation of transdermal patches containing risperidone (pp. 39-50) https://doi.org/10.3109/03639045.2012.657643
- Al-Achi et al. (2013) Wiley
- Ale et al. (2009) Skin tolerability associated with transdermal drug delivery systems: an overview (pp. 920-935) https://doi.org/10.1007/s12325-009-0075-9
- Anderson et al. (2002) Time course of lamotrigine de-induction: impact of stepwise withdrawal of carbamazepine or phenytoin (pp. 211-217) https://doi.org/10.1016/S0920-1211(02)00033-5
- Arora and Mukherjee (2002) Design, development, physicochemical, and in vitro and in vivo evaluation of transdermal patches containing diclofenac diethylammonium salt (pp. 2076-2089) https://doi.org/10.1002/jps.10200
- Levy et al. (2002) Lippincott Williams and Wilkins
- Costa and Lobo (2001) Modeling and comparison of dissolution profiles (pp. 123-133) https://doi.org/10.1016/S0928-0987(01)00095-1
- Costa and Sousa Lobo (2003) Evaluation of mathematical models describing drug release from estradiol transdermal systems (pp. 89-97) https://doi.org/10.1081/DDC-120016687
- Draize et al. (1944) Methods for the study of irritation and toxicity of substances applied topically to the skin and mucous membranes (pp. 377-390)
- Francoeur et al. (1990) Oleic acid: its effects on stratum corneum in relation to (trans) dermal drug delivery (pp. 621-627) https://doi.org/10.1023/A:1015822312426
- Gannu et al. (2007) Development of nitrendipine transdermal patches: in vitro and ex vivo characterization (pp. 69-76) https://doi.org/10.2174/156720107779314767
- Gidal et al. (2000) Lack of an effect of valproate concentration on lamotrigine pharmacokinetics in developmentally disabled patients with epilepsy (pp. 23-31) https://doi.org/10.1016/S0920-1211(00)00160-1
- Guyot and Fawaz (2000) Design and in vitro evaluation of adhesive matrix for transdermal delivery of propranolol (pp. 171-182) https://doi.org/10.1016/S0378-5173(00)00494-4
- Hillery and Park (2016) CRC Press https://doi.org/10.1201/9781315382579
- Jiang (2017) Development of essential oils as skin permeation enhancers: penetration enhancement effect and mechanism of action (pp. 1592-1600) https://doi.org/10.1080/13880209.2017.1312464
- Kalia and Guy (2001) Modeling transdermal drug release (pp. 159-172) https://doi.org/10.1016/S0169-409X(01)00113-2
- Karande et al. (2006) Insights into synergistic interactions in binary mixtures of chemical permeation enhancers for transdermal drug delivery (pp. 85-93) https://doi.org/10.1016/j.jconrel.2006.07.001
- Kusum Devi et al. (2003) Design and evaluation of matrix diffusion controlled transdermal patches of verapamil hydrochloride (pp. 495-503) https://doi.org/10.1081/DDC-120018638
- Leach et al. (1986) Pharmacological studies on lamotrigine, a novel potential antiepileptic drug (pp. 490-497) https://doi.org/10.1111/j.1528-1157.1986.tb03573.x
- Minghetti et al. (2007) Evaluation of the topical anti-inflammatory activity of ginger dry extracts from solutions and plasters 73(15) (pp. 1525-1530) https://doi.org/10.1055/s-2007-993741
- Misra (2014) Smithers Rapra Technology Ltd
- Mukherjee et al. (2005) A comparison between povidone-ethylcellulose and povidone-eudragit transdermal dexamethasone matrix patches based on in vitro skin permeation (pp. 475-483) https://doi.org/10.1016/j.ejpb.2004.09.009
- Naik et al. (1995) Mechanism of oleic acid-induced skin penetration enhancement in vivo in humans (pp. 299-306) https://doi.org/10.1016/0168-3659(95)00088-7
- Prajapati et al. (2011) Formulation and evaluation of transdermal patch of repaglinide https://doi.org/10.5402/2011/651909
- Prasad Verma and Chandak (2009) Development of matrix controlled transdermal delivery systems of pentazocine: in vitro/in vivo performance (pp. 171-186) https://doi.org/10.2478/v10007-009-0014-y
- Prausnitz and Langer (2008) Transdermal drug delivery (pp. 1261-1268) https://doi.org/10.1038/nbt.1504
- Prausnitz et al. (2004) Current status and future potential of transdermal drug delivery (pp. 115-124) https://doi.org/10.1038/nrd1304
- Rajabalaya (2010) Studies on effect of plasticizer on invitro release and exvivo permeation from eudragit e100 based chlorpheniramine maleate matrix type transdermal delivery system (pp. 3-12)
- Rajan et al. (2009) Design and in vitro evaluation of chlorpheniramine maleate from different eudragit based matrix patches: effect of platicizer and chemical enhancers 50(4) (pp. 177-194)
- Rambeck and Wolf (1993) Lamotrigine clinical pharmacokinetics (pp. 433-443) https://doi.org/10.2165/00003088-199325060-00003
- Shinde et al. (2008) Development and characterization of transdermal therapeutics system of tramadol hydrochloride https://doi.org/10.4103/0973-8398.45044
- Touitou et al. (2002) Oleic acid, a skin penetration enhancer, affects Langerhans cells and corneocytes (pp. 1-7) https://doi.org/10.1016/S0168-3659(02)00004-4
- Ubaidulla et al. (2007) Transdermal therapeutic system of carvedilol: effect of hydrophilic and hydrophobic matrix on in vitro and in vivo characteristics (pp. E13-E20) https://doi.org/10.1208/pt0801002
- Valenta and Auner (2004) The use of polymers for dermal and transdermal delivery (pp. 279-289) https://doi.org/10.1016/j.ejpb.2004.02.017
- Venkatraman and Gale (1998) Skin adhesives and skin adhesion: 1. Transdermal drug delivery systems (pp. 1119-1136) https://doi.org/10.1016/S0142-9612(98)00020-9
- Wade and Weller (1994) American Pharmaceutical Association
- Wang et al. (2008) Development and evaluation of the Sinomenine transdermal patch (pp. 407-410)
- Williams and Barry (2012) Penetration enhancers (pp. 128-137) https://doi.org/10.1016/j.addr.2012.09.032
- Yuen et al. (1992) Sodium valproate acutely inhibits lamotrigine metabolism (pp. 511-513) https://doi.org/10.1111/j.1365-2125.1992.tb04079.x
- Zhang et al. (2010) DDSolver: an add-in program for modeling and comparison of drug dissolution profiles (pp. 263-271) https://doi.org/10.1208/s12248-010-9185-1
10.1007/s40204-019-0114-9