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Current Drug Therapy

Editor-in-Chief

ISSN (Print): 1574-8855
ISSN (Online): 2212-3903

Research Article

Enhancement of Drug Penetration Rate by Enriching Skin Hydration: A Novel Amalgamation of Microemulsion and Supersaturation

Author(s): Dipika Chavda*, Atindra Shukla and Tejal Soni

Volume 17, Issue 2, 2022

Published on: 30 March, 2022

Page: [118 - 131] Pages: 14

DOI: 10.2174/1574885517666220330141528

Price: $65

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Abstract

Background: The evolving need and facilitation of topical formulations have risen in the present era. Topical industries are continually striving to satisfy patients with newer and innovative products. However, dry skin is the critical factor contributing to drug penetration into the skin.

Objectives: The current research aims to develop cost-effective and commercially feasible industrial scale microemulsion of wheat germ oil to enrich skin hydration, enhancing the drug permeation rate.

Methods: The Pseudo-ternary phase diagram was constructed for screening of microemulsion components. Wheat germ oil containing O/W microemulsion was prepared and evaluated for physicochemical parameters, thermodynamic stability study, globule size determination, enhancement of skin hydration, and skin permeation rate by ex vivo study.

Results: The wheat germ oil containing microemulsion was prepared by incorporating tween 20 [surfactant] and ethanol [co-surfactant]. All physicochemical parameters were in the ideal range. Following the thermodynamic stability study, the TEM study showed globule size of optimized microemulsions in the range of 69.64 nm to 84.42 nm. The skin moisture tester showed a high hydration level for more than eight hours. An Ex vivo study revealed higher drug flux [Jss] of Pomegranate peel Extract [17.99 μg/cm2/h] with an enhancement ratio of 1.69.

Conclusion: The topical formulation application has become challenging for researchers due to the skin's dryness and lower water content. However, the developed WGO microemulsion aids more penetration and is helpful in achieving higher drug flux. In addition, it is a cost-effective, easy to prepare, and patient-friendly drug delivery system.

Keywords: Microemulsion, dry skin, wheat germ oil, skin moisture tester, drug penetration, pomegranate peel extract, skin hydration, amalgamation, supersaturation.

Graphical Abstract

[1]
Hikima T, Maibach H. Skin penetration flux and lag-time of steroids across hydrated and dehydrated human skin in vitro. Biol Pharm Bull 2006; 29(11): 2270-3.
[http://dx.doi.org/10.1248/bpb.29.2270] [PMID: 17077527]
[2]
Parhi R, Suresh P, Mondal S, Kumar PM. Novel penetration enhancers for skin applications: A review. Curr Drug Deliv 2012; 9(2): 219-30.
[http://dx.doi.org/10.2174/156720112800234585] [PMID: 22023208]
[3]
Haque T, Talukder MMU. Chemical enhancer: A simplistic way to modulate barrier function of the stratum corneum. Adv Pharm Bull 2018; 8(2): 169-79.
[http://dx.doi.org/10.15171/apb.2018.021] [PMID: 30023318]
[4]
Kwan P, Sills GJ, Brodie MJ. Understanding the role of NMF in skin hydration. Pract Dermatol 2012; (1): 21-34.
[http://dx.doi.org/10.1016/S0163-7258(01)00122-X]
[5]
Ruela LAM, Perissinato AG, de Sousa Lino ME, Nudrik PS. Perrera, GR. Evaluation of skin absorption of drugs from topical and transdermal formulations. Braz J Pharm Sci 2016; 50(3): 52.
[6]
Benson HAE. Transdermal drug delivery: Penetration enhancement techniques. Curr Drug Deliv 2005; 2(1): 23-33.
[http://dx.doi.org/10.2174/1567201052772915] [PMID: 16305405]
[7]
Potts RO, Buras EM Jr, Chrisman DA Jr. Changes with age in the moisture content of human skin. J Invest Dermatol 1984; 82(1): 97-100.
[http://dx.doi.org/10.1111/1523-1747.ep12259203] [PMID: 6690633]
[8]
Werschler WP, Trookman NS, Rizer RL, Ho ET, Mehta R. Enhanced efficacy of a facial hydrating serum in subjects with normal or self-perceived dry skin. J Clin Aesthet Dermatol 2011; 4(2): 51-5.
[PMID: 21386958]
[9]
EFSA Panel on Dietetic Products. EFSA Panel on dietetic products, nutrition and allergies (NDA) scientific opinion on the substantiation of health claims related to guar gum and maintenance of normal blood glucose concentrations [ID 794], increase in satiety [ID 795] and maintenance of normal blood cholesterol concentrations. EFSA J Eur Food Safety Authority 2010; 8(2): 1464.
[10]
Kumar GS, Krishna AGG. Studies on the nutraceuticals composition of wheat derived oils wheat bran oil and wheat germ oil. J Food Sci Technol 2015; 52(2): 1145-51.
[http://dx.doi.org/10.1007/s13197-013-1119-3] [PMID: 25694731]
[11]
van den Bosch MHJ. Inflammation in osteoarthritis: Is it time to dampen the alarm(in) in this debilitating disease? Clin Exp Immunol 2019; 195(2): 153-66.
[http://dx.doi.org/10.1111/cei.13237] [PMID: 30421798]
[12]
Johnston SA. Osteoarthritis. Joint anatomy, physiology, and pathobiology. Vet Clin North Am Small Anim Pract 1997; 27(4): 699-723.
[http://dx.doi.org/10.1016/S0195-5616(97)50076-3] [PMID: 9243777]
[13]
Park H, Ha ES, Kim MS. Current status of supersaturable self-emulsifying drug delivery systems. Pharmaceutics 2020; 12(4): 365.
[http://dx.doi.org/10.3390/pharmaceutics12040365] [PMID: 32316199]
[14]
Moser K, Kriwet K, Kalia YN, Guy RH. Enhanced skin permeation of a lipophilic drug using supersaturated formulations. J Control Release 2001; 73(2-3): 245-53.
[http://dx.doi.org/10.1016/S0168-3659(01)00290-5] [PMID: 11516502]
[15]
Joshi P, Sangamwar AT. Stabilizing supersaturated drug-delivery system through mechanism of nucleation and crystal growth inhibition of drugs. Ther Deliv 2018; 9(12): 873-85.
[http://dx.doi.org/10.4155/tde-2018-0031] [PMID: 30444454]
[16]
Chaudhari SP, Dave RH. Evaluating the effects of different molecular weights of polymers in stabilizing supersaturated drug solutions and formulations using various methodologies of the model drug: Fenofibrate. J Pharm Sci Pharmacol 2016; 2(3): 259-76.
[http://dx.doi.org/10.1166/jpsp.2015.1066]
[17]
Mastrogiovanni F, Mukhopadhya A, Lacetera N, et al. Anti-inflammatory effects of pomegranate peel extracts on in vitro human intestinal caco-2 cells and ex vivo porcine colonic tissue explants. Nutrients 2019; 11(3): 1-15.
[http://dx.doi.org/10.3390/nu11030548] [PMID: 30841512]
[18]
Ismail T, Sestili P, Akhtar S. Pomegranate peel and fruit extracts: A review of potential anti-inflammatory and anti-infective effects. J Ethnopharmacol 2012; 143(2): 397-405.
[http://dx.doi.org/10.1016/j.jep.2012.07.004] [PMID: 22820239]
[19]
Bhandary S, Sharmila KP, Kumari NS, Bhat VS. Assessment of anti- inflammatory activity of Punica granatum L. ethanol extracts and synthetic ellagic acid in swiss albino mice. Am J Pharm Health Res 2014; 2(4): 1-12.
[20]
Yadav V, Jadhav P, Kanase K, Bodhe A, Dombe S. Preparation and evaluation of microemulsion containing antihypertensive drug. Int J Appl Pharm 2018; 10(5): 138-46.
[http://dx.doi.org/10.22159/ijap.2018v10i5.27415]
[21]
Patel TB, Patel TR, Suhagia BN. Preparation, characterization, and optimization of microemulsion for topical delivery of itraconazole. J Drug Deliv Ther 2018; 8(2): 136-45.
[http://dx.doi.org/10.22270/jddt.v8i2.1731]
[22]
Azeem A, Rizwan M, Ahmad FJ, et al. Emerging role of microemulsions in cosmetics. Recent Pat Drug Deliv Formul 2008; 2(3): 275-89.
[http://dx.doi.org/10.2174/187221108786241624] [PMID: 19075913]
[23]
Basheer HS, Noordin MI, Ghareeb MM. Characterization of microemulsions prepared using isopropyl palmitate with various surfactants and cosurfactants. Trop J Pharm Res 2013; 12(3): 305-10.
[http://dx.doi.org/10.4314/tjpr.v12i3.5]
[24]
Zhao J, Jiang K, Chen Y, et al. Preparation and characterization of microemulsions based on antarctic krill oil. Mar Drugs 2020; 18(10): 492.
[http://dx.doi.org/10.3390/md18100492] [PMID: 32993042]
[25]
Mathews CDC, Sugano K. Supersaturable formulations. Drug Deliv Syst 2010; 25(4): 371-4.
[http://dx.doi.org/10.2745/dds.25.371]
[26]
Nayak AK, Panigrahi PP. Solubility enhancement of etoricoxib by cosolvency approach. Int Scholar Res Notices Phys Chem 2012; 2012: 1-5.
[27]
Vandecruys R, Peeters J, Verreck G, Brewster ME. Use of a screening method to determine excipients which optimize the extent and stability of supersaturated drug solutions and application of this system to solid formulation design. Int J Pharm 2007; 342(1-2): 168-75.
[http://dx.doi.org/10.1016/j.ijpharm.2007.05.006] [PMID: 17573214]
[28]
Blaabjerg LI, Grohganz H, Lindenberg E, Löbmann K, Müllertz A, Rades T. The influence of polymers on the supersaturation potential of poor and good glass formers. Pharmaceutics 2018; 10(4): 164.
[http://dx.doi.org/10.3390/pharmaceutics10040164] [PMID: 30241425]
[29]
Quan G, Niu B, Singh V, et al. Supersaturable solid self-microemulsifying drug delivery system: Precipitation inhibition and bioavailability enhancement. Int J Nanomedicine 2017; 12: 8801-11.
[http://dx.doi.org/10.2147/IJN.S149717] [PMID: 29263669]
[30]
Schultz HB, Thomas N, Rao S, Prestidge CA. Supersaturated silica-lipid hybrids (super-SLH): An improved solid-state lipid-based oral drug delivery system with enhanced drug loading. Eur J Pharm Biopharm 2018; 125: 13-20.
[http://dx.doi.org/10.1016/j.ejpb.2017.12.012] [PMID: 29277724]
[31]
Tartaro G, Mateos H, Schirone D, Angelico R, Palazzo G. Microemulsion microstructure[s]: A tutorial review. Nanomaterials (Basel) 2020; 10(9): 1657.
[http://dx.doi.org/10.3390/nano10091657] [PMID: 32846957]
[32]
Kathe K, Kathpalia H. Film forming systems for topical and transdermal drug delivery. Asian J Pharm Sci 2017; 12(6): 487-97.
[http://dx.doi.org/10.1016/j.ajps.2017.07.004] [PMID: 32104362]
[33]
Mori NM, Patel P, Sheth NR, Rathod LV, Ashara KC. Fabrication and characterization of film-forming voriconazole transdermal spray for the treatment of fungal infection. Bull Fac Pharm Cairo Univ 2017; 55(1): 41-51.
[http://dx.doi.org/10.1016/j.bfopcu.2017.01.001]
[34]
Patil UK, Saraogi R. Natural products as potential drug permeation enhancer in transdermal drug delivery system. Arch Dermatol Res 2014; 306(5): 419-26.
[http://dx.doi.org/10.1007/s00403-014-1445-y] [PMID: 24481830]
[35]
Constantin MM, Poenaru E, Poenaru C, Constantin T. Skin hydration assessment through modern non-invasive bioengineering technologies. Maedica (Buchar) 2014; 9(1): 33-8.
[PMID: 25553123]
[36]
Chen Y, Quan P, Liu X, Wang M, Fang L. Novel chemical permeation enhancers for transdermal drug delivery. Asian J Pharm Sci 2014; 9(2): 51-64.
[http://dx.doi.org/10.1016/j.ajps.2014.01.001]
[37]
Sawatdee S, Choochuay K, Chanthorn W, Srichana T. Evaluation of the topical spray containing Centella asiatica extract and its efficacy on excision wounds in rats. Acta Pharm 2016; 66(2): 233-44.
[http://dx.doi.org/10.1515/acph-2016-0018] [PMID: 27279066]
[38]
Azeem A, Rizwan M, Ahmad FJ, et al. Nanoemulsion components screening and selection: A technical note. AAPS PharmSciTech 2009; 10(1): 69-76.
[http://dx.doi.org/10.1208/s12249-008-9178-x] [PMID: 19148761]
[39]
Shen LN, Zhang YT, Wang Q, Xu L, Feng NP. Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of Rhizoma arisaematis. Int J Nanomedicine 2014; 9(1): 3453-64.
[PMID: 25092976]

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