Enhanced penetration strategies for transdermal delivery
Tóm tắt
Transdermal delivery offers several advantages in drug distribution, including convenience, painless administration, avoidance of first-pass metabolism, and ease of termination. However, the natural protective barriers of the skin, such as the stratum corneum, the topmost layer of skin, limit the systemic absorption of external therapeutics via transdermal delivery. Therefore, extensive application of transdermal delivery in medical treatment has been limited. Over the past few years, many formulation strategies and physical technologies, therefore, have been developed to enhance transdermal delivery. This review summarizes various formulation strategies proposed for transdermal delivery and their application in medical treatment.
Tài liệu tham khảo
Jin J F, Zhu L L, Xu H M, Wang H F, Feng X Q, Zhu X P, Zhou Q. The optimal choice of medication administration route regarding intravenous, intramuscular, and subcutaneous injection. Patient Preference and Adherence, 2015, 9: 923–942
Rowland M. Influence of route of administration on drug availability. Journal of Pharmaceutical Sciences, 1972, 61(1): 70–74
Duchene D, Touchard F, Peppas N. Pharmaceutical and medical aspects of bioadhesive systems for drug administration. Drug Development and Industrial Pharmacy, 1988, 14(2-3): 283–318
Prausnitz M R, Langer R. Transdermal drug delivery. Nature Biotechnology, 2008, 26(11): 1261–1268
Prausnitz M R, Mitragotri S, Langer R. Current status and future potential of transdermal drug delivery. Nature Reviews. Drug Discovery, 2004, 3(2): 115–124
Kalluri H, Banga A K. Transdermal delivery of proteins. AAPS PharmSciTech, 2011, 12(1): 431–441
Carter P, Narasimhan B, Wang Q. Biocompatible nanoparticles and vesicular systems in transdermal drug delivery for various skin diseases. International Journal of Pharmaceutics, 2019, 555: 49–62
Alkilani A, McCrudden M T, Donnelly R. Transdermal drug delivery: Innovative pharmaceutical developments based on disruption of the barrier properties of the stratum corneum. Pharmaceutics, 2015, 7(4): 438–470
Chen Y, Shen Y, Guo X, Zhang C, Yang W, Ma M, Liu S, Zhang M, Wen L P. Transdermal protein delivery by a coadministered peptide identified via phage display. Nature Biotechnology, 2006, 24(4): 455–460
Lopes L B, Garcia M T J, Bentley M V L. Chemical penetration enhancers. Therapeutic Delivery, 2015, 6(9): 1053–1061
Chen Y, Quan P, Liu X, Wang M, Fang L. Novel chemical permeation enhancers for transdermal drug delivery. Asian Journal of Pharmaceutical Sciences, 2014, 9(2): 51–64
Pham Q D, Björklund S, Engblom J, Topgaard D, Sparr E. Chemical penetration enhancers in stratum corneum—relation between molecular effects and barrier function. Journal of Controlled Release, 2016, 232: 175–187
Tscheik C, Blasig I E, Winkler L. Trends in drug delivery through tissue barriers containing tight junctions. Tissue Barriers, 2013, 1 (2): e24565
Pathan I B, Setty C M. Chemical penetration enhancers for transdermal drug delivery systems. Tropical Journal of Pharmaceutical Research, 2009, 8(2): 173–179
Karande P, Jain A, Ergun K, Kispersky V, Mitragotri S. Design principles of chemical penetration enhancers for transdermal drug delivery. Proceedings of the National Academy of Sciences of the United States of America, 2005, 102(13): 4688–4693
Haque T, Talukder M M U. Chemical Enhancer: A simplistic way to modulate barrier function of the stratum corneum. Advanced Pharmaceutical Bulletin, 2018, 8(2): 169–179
Ibrahim S A, Li S K. Efficiency of fatty acids as chemical penetration enhancers: Mechanisms and structure enhancement relationship. Pharmaceutical Research, 2010, 27(1): 115–125
Lane M E. Skin penetration enhancers. International Journal of Pharmaceutics, 2013, 447(1-2): 12–21
Kandimalla K, Kanikkannan N, Andega S, Singh M. Effect of Fatty acids on the permeation of melatonin across rat and pig skin in-vitro and on the transepidermal water loss in rats in-vivo. Journal of Pharmacy and Pharmacology, 1999, 51(7): 783–790
Aungst B J J, Rogers N, Shefter E. Enhancement of naloxone penetration through human skin in vitro using fatty acids, fatty alcohols, surfactants, sulfoxides and amides. International Journal of Pharmaceutics, 1986, 33(1): 225–234
Aungst B J. Structure/Effect studies of fatty acid isomers as skin penetration enhancers and skin irritants. Pharmaceutical Research, 1989, 6(3): 244–247
Ongpipattanakul B, Burnette R R, Potts R O, Francoeur M L. Evidence that oleic acid exists in a separate phase within stratum corneum lipids. Pharmaceutical Research, 1991, 8(3): 350–354
Babu R J, Chen L, Kanikkannan N. Fatty alcohols, fatty acids, and fatty acid esters as penetration enhancers. Springer Berlin Heidelberg location: Springer Berlin Heidelberg, 2015, 133–150
Parivesh S, Sumeet D, Abhishek D. Design, evaluation, parameters and marketed products of transdermal patches: A review. Journal of Pharmacy Research, 2010, 3(2): 235–240
Jordan W P Jr, Atkinson L E, Lai C. Comparison of the skin irritation potential of two testosterone transdermal systems: An investigational system and a marketed product. Clinical Therapeutics, 1998, 20(1): 80–87
Williams A C, Barry B W. Penetration enhancers. Advanced Drug Delivery Reviews, 2012, 64(Suppl): 128–137
Liu P, Cettina M, Wong J. Effects of isopropanol-isopropyl myristate binary enhancers on in vitro transport of estradiol in human epidermis: A mechanistic evaluation. Journal of Pharmaceutical Sciences, 2009, 98(2): 565–572
Watkinson R M, Herkenne C, Guy R H, Hadgraft J, Oliveira G, Lane M E. Influence of ethanol on the solubility, ionization and permeation characteristics of Ibuprofen in silicone and human skin. Skin Pharmacology and Physiology, 2009, 22(1): 15–21
Wischke C, Schwendeman S P. Principles of encapsulating hydrophobic drugs in PLA/PLGA microparticles. International Journal of Pharmaceutics, 2008, 364(2): 298–327
Andega S, Kanikkannan N, Singh M. Comparison of the effect of fatty alcohols on the permeation of melatonin between porcine and human skin. Journal of Controlled Release, 2001, 77(1): 17–25
Dias M, Naik A, Guy R H, Hadgraft J, Lane M E. In vivo infrared spectroscopy studies of alkanol effects on human skin. European Journal of Pharmaceutics and Biopharmaceutics, 2008, 69(3): 1171–1175
Jampilek J, Brychtova K. Azone analogues: Classification, design, and transdermal penetration principles. Medicinal Research Reviews, 2012, 32(5): 907–947
Harrison J E, Watkinson A C, Green DM, Hadgraft J, Brain K. The relative effect of azone and transcutol on permeant diffusivity and solubility in human stratum corneum. Pharmaceutical Research, 1996, 13(4): 542–546
Harrison J E, Groundwater P W, Brain K R, Hadgraft J. Azone® induced fluidity in human stratum corneum. A fourier transform infrared spectroscopy investigation using the perdeuterated analogue. Journal of Controlled Release, 1996, 41(3): 283–290
Hadgraft J. Passive enhancement strategies in topical and transdermal drug delivery. International Journal of Pharmaceutics, 1999, 184(1): 1–6
Hadgraft J, Peck J, Williams D G, PughWJ, Allan G. Mechanisms of action of skin penetration enhancers/retarders: Azone and analogues. International Journal of Pharmaceutics, 1996, 141(1): 17–25
Zou L L, Ma J L, Wang T, Yang T B, Liu C B. Cell-penetrating peptide-mediated therapeutic molecule delivery into the central nervous system. Current Neuropharmacology, 2013, 11(2): 197–208
Stalmans S, Bracke N, Wynendaele E, Gevaert B, Peremans K, Burvenich C, Polis I, De Spiegeleer B. Cell-penetrating peptides selectively cross the blood-brain barrier in vivo. PLoS One, 2015, 10(10): e0139652
Liu X, Zhang P, Rödl W, Maier K, Lächelt U, Wagner E. Toward artificial immunotoxins: Traceless reversible conjugation of RNase A with receptor targeting and endosomal escape domains. Molecular Pharmaceutics, 2017, 14(5): 1439–1449
Wagner E, Zenke M, Cotten M, Beug H, Birnstiel M L. Transferrin-polycation conjugates as carriers for DNA uptake into cells. Proceedings of the National Academy of Sciences of the United States of America, 1990, 87(9): 3410–3414
Schwarze S R, Ho A, Vocero-Akbani A, Dowdy S F. In vivo protein transduction: Delivery of a biologically active protein into the mouse. Science, 1999, 285(5433): 1569–1572
Erazo-Oliveras A, Najjar K, Dayani L, Wang T Y, Johnson G A, Pellois J P. Protein delivery into live cells by incubation with an endosomolytic agent. Nature Methods, 2014, 11(8): 861–867
Kamada H, Okamoto T, Kawamura M, Shibata H, Abe Y, Ohkawa A, Nomura T, Sato M, Mukai Y, Sugita T, et al. Creation of novel cell-penetrating peptides for intracellular drug delivery using systematic phage display technology originated from Tat transduction domain. Biological & Pharmaceutical Bulletin, 2007, 30(2): 218–223
Tang H, Yin L, Kim K H, Cheng J. Helical poly(arginine) mimics with superior cell-penetrating and molecular transporting properties. Chemical Science (Cambridge), 2013, 4(10): 3839–3844
Lozano M V, Lollo G, Alonso-Nocelo M, Brea J, Vidal A, Torres D, Alonso M J. Polyarginine nanocapsules: A new platform for intracellular drug delivery. Journal of Nanoparticle Research, 2013, 15(3): 1515
Rothbard J B, Garlington S, Lin Q, Kirschberg T, Kreider E, McGrane P L, Wender P A, Khavari P A. Conjugation of arginine oligomers to cyclosporin A facilitates topical delivery and inhibition of inflammation. Nature Medicine, 2000, 6(11): 1253–1257
Kim Y C, Ludovice P J, Prausnitz M R. Transdermal delivery enhanced by magainin pore-forming peptide. Journal of Controlled Release, 2007, 122(3): 375–383
Jung E, Lee J, Park J, Park D. Transdermal delivery of interferon-γ (IFN-γ) mediated by penetratin, a cell-permeable peptide. Biotechnology and Applied Biochemistry, 2005, 42(2): 169–173
Hsu T, Mitragotri S. Delivery of siRNA and other macromolecules into skin and cells using a peptide enhancer. Proceedings of the National Academy of Sciences of the United States of America, 2011, 108(38): 15816–15821
Lin C M, Huang K, Zeng Y, Chen X C, Wang S, Li Y. A simple, noninvasive and efficient method for transdermal delivery of siRNA. Archives of Dermatological Research, 2012, 304(2): 139–144
Candan G, Michiue H, Ishikawa S, Fujimura A, Hayashi K, Uneda A, Mori A, Ohmori I, Nishiki T I, Matsui H, Tomizawa K. Combining poly-arginine with the hydrophobic counter-anion 4-(1-pyrenyl)-butyric acid for protein transduction in transdermal delivery. Biomaterials, 2012, 33(27): 6468–6475
Gautam A, Nanda J S, Samuel J S, Kumari M, Priyanka P, Bedi G, Nath S K, Mittal G, Khatri N, Raghava G P S. Topical delivery of protein and peptide esing novel cell penetrating peptide IMT-P8. Scientific Reports, 2016, 6(1): 26278
Zhang T, Qu H, Li X, Zhao B, Zhou J, Li Q, Sun M. Transmembrane delivery and biological effect of human growth hormone via a phage displayed peptide in vivo and in vitro. Journal of Pharmaceutical Sciences, 2010, 99(12): 4880–4891
Chang M, Li X, Sun Y, Cheng F,Wang Q, Xie X, Zhao W, Tian X. Effect of cationic cyclopeptides on transdermal and transmembrane delivery of insulin. Molecular Pharmaceutics, 2013, 10(3): 951–957
Cevc G, Blume G. New, highly efficient formulation of diclofenac for the topical, transdermal administration in ultradeformable drug carriers, Transfersomes. Biochimica et Biophysica Acta (BBA)-. Biomembranes, 2001, 1514(2): 191–205
Cevc G, Schätzlein A, Blume G. Transdermal drug carriers: Basic properties, optimization and transfer efficiency in the case of epicutaneously applied peptides. Journal of Controlled Release, 1995, 36(1): 3–16
Al Shuwaili A H, Rasool B K A, Abdulrasool A A. Optimization of elastic transfersomes formulations for transdermal delivery of pentoxifylline. European Journal of Pharmaceutics and Biopharmaceutics, 2016, 102: 101–114
Benson H A. Transfersomes for transdermal drug delivery. Expert Opinion on Drug Delivery, 2006, 3(6): 727–737
Jain S, Jain P, Umamaheshwari R, Jain N. Transfersomes—a novel vesicular carrier for enhanced transdermal delivery: Development, characterization, and performance evaluation. Drug Development and Industrial Pharmacy, 2003, 29(9): 1013–1026
Cevc G. Transdermal drug delivery of insulin with ultradeformable carriers. Clinical Pharmacokinetics, 2003, 42(5): 461–474
Rai S, Pandey V, Rai G. Transfersomes as versatile and flexible nano-vesicular carriers in skin cancer therapy: The state of the art. Nano Reviews & Experiments, 2017, 8(1): 1325708
Wang J, Wei Y, Fei Y R, Fang L, Zheng H S, Mu C F, Li F Z, Zhang Y S. Preparation of mixed monoterpenes edge activated PEGylated transfersomes to improve the in vivo transdermal delivery efficiency of sinomenine hydrochloride. International Journal of Pharmaceutics, 2017, 533(1): 266–274
Liu J, Li W, Teng H, Lin Z. Immunopharmacological action of sinomenine, an alkaloid isolated from Sinomenium acutum, and its mechanism of action in treating rheumatoid arthritis. Acta Pharmaceutica Sinica, 2005, 40(2): 127–131 (in Chinese)
Feng H, Yamaki K, Takano H, Inoue K, Yanagisawa R, Yoshino S. Effect of sinomenine on collagen-induced arthritis in mice. Autoimmunity, 2007, 40(7): 532–539
Han W, Li W, Wang X, Zhang H, Sun Y, Hao B. Preparation of sinomenine hydrochloride loaded nano flexible liposomes and their characteristics. Chinese Traditional and Herbal Drugs, 2011, 42(4): 671–675 (in Chinese)
Ward A, Clissold S P. Pentoxifylline. Drugs, 1987, 34(1): 50–97
Smith R V, Waller E S, Doluisio J T, Bauza M T, Puri S K, Ho I, Lassman H B. Pharmacokinetics of orally administered pentoxifylline in humans. Journal of Pharmaceutical Sciences, 1986, 75(1): 47–52
Rames A, Poirier JM, LeCoz F, Midavaine M, Lecocq B, Grange J D, Poupon R, Cheymol G, Jaillon P. Pharmacokinetics of intravenous and oral pentoxifylline in healthy volunteers and in cirrhotic patients. Clinical Pharmacology and Therapeutics, 1990, 47(3): 354–359
Bryce T, Chamberlain J, Hillbeck D, Macdonald C. Metabolism and pharmacokinetics of 14C-pentoxifylline in healthy volunteers. Arzneimittel-Forschung, 1989, 39(4): 512–517
Jiang T, Wang T, Li T, Ma Y, Shen S, He B, Mo R. Enhanced transdermal drug delivery by transfersome-embedded oligopeptide hydrogel for topical chemotherapy of melanoma. ACS Nano, 2018, 12(10): 9693–9701
Bangham A D, Horne R. Negative staining of phospholipids and their structural modification by surface-active agents as observed in the electron microscope. Journal of Molecular Biology, 1964, 8(5): 660–668
Petersen A L, Hansen A E, Gabizon A, Andresen T L. Liposome imaging agents in personalized medicine. Advanced Drug Delivery Reviews, 2012, 64(13): 1417–1435
Zhang P, He D, Klein P M, Liu X, Röder R, Döblinger M, Wagner E. Enhanced intracellular protein transduction by sequence defined tetra-oleoyl oligoaminoamides targeted for cancer therapy. Advanced Functional Materials, 2015, 25(42): 6627–6636
Eloy J O, Claro de Souza M, Petrilli R, Barcellos J P A, Lee R J, Marchetti J M. Liposomes as carriers of hydrophilic small molecule drugs: Strategies to enhance encapsulation and delivery. Colloids and Surfaces. B, Biointerfaces, 2014, 123: 345–363
Duong A D, Collier M A, Bachelder E M, Wyslouzil B E, Ainslie K M. One step encapsulation of small molecule drugs in liposomes via electrospray-remote loading. Molecular Pharmaceutics, 2016, 13(1): 92–99
Huwyler J, Wu D, Pardridge W M. Brain drug delivery of small molecules using immunoliposomes. Proceedings of the National Academy of Sciences of the United States of America, 1996, 93 (24): 14164–14169
Gregoriadis G, Neerunjun D E. Control of the rate of hepatic uptake and catabolism of liposome-entrapped proteins injected into rats. Possible therapeutic applications. European Journal of Biochemistry, 1974, 47(1): 179–185
Tan M L, Choong P F, Dass C R. Recent developments in liposomes, microparticles and nanoparticles for protein and peptide drug delivery. Peptides, 2010, 31(1): 184–193
Chatin B, Mével M, Devallière J, Dallet L, Haudebourg T, Peuziat P, Colombani T, Berchel M, Lambert O, Edelman A, Pitard B. Liposome-based formulation for intracellular delivery of functional proteins. Molecular Therapy. Nucleic Acids, 2015, 4: e244
Rahimpour Y, Hamishehkar H. Liposomes in cosmeceutics. Expert Opinion on Drug Delivery, 2012, 9(4): 443–455
Sacha M, Faucon L, Hamon E, Ly I, Haltner-Ukomadu E. Ex vivo transdermal absorption of a liposome formulation of diclofenac. Biomedicine and Pharmacotherapy, 2019, 111: 785–790
Yang G, Lee H E, Shin S W, Um S H, Lee J D, Kim K B, Kang H C, Cho Y Y, Lee H S, Lee J Y. Efficient transdermal delivery of DNA nanostructures alleviates atopic dermatitis symptoms in NC/Nga mice. Advanced Functional Materials, 2018, 28(40): 1801918
Yamazaki N, Sugimoto T, Fukushima M, Teranishi R, Kotaka A, Shinde C, Kumei T, Sumida Y, Munekata Y, Maruyama K I, et al. Dual-stimuli responsive liposomes using pH- and temperaturesensitive polymers for controlled transdermal delivery. Polymer Chemistry, 2017, 8(9): 1507–1518
Donnelly R F, Singh T R R, Woolfson A D. Microneedle-based drug delivery systems: Microfabrication, drug delivery, and safety. Drug Delivery, 2010, 17(4): 187–207
Larrañeta E, McCrudden M T C, Courtenay A J, Donnelly R F. Microneedles: A new frontier in nanomedicine delivery. Pharmaceutical Research, 2016, 33(5): 1055–1073
Liu X, Wang C, Liu Z. Protein-engineered biomaterials for cancer theranostics. Advanced Healthcare Materials, 2018, 7(20): 1800913
Ye Y, Yu J, Wen D, Kahkoska A R, Gu Z. Polymeric microneedles for transdermal protein delivery. Advanced Drug Delivery Reviews, 2018, 127: 106–118
Waghule T, Singhvi G, Dubey S K, Pandey M M, Gupta G, Singh M, Dua K. Microneedles: A smart approach and increasing potential for transdermal drug delivery system. Biomedicine and Pharmacotherapy, 2019, 109: 1249–1258
Larrañeta E, Lutton R E M, Woolfson A D, Donnelly R F. Microneedle arrays as transdermal and intradermal drug delivery systems: Materials science, manufacture and commercial development. Materials Science and Engineering R Reports, 2016, 104: 1–32
Moffatt K, Wang Y, Raj Singh T R, Donnelly R F. Microneedles for enhanced transdermal and intraocular drug delivery. Current Opinion in Pharmacology, 2017, 36: 14–21
McGrath M G, Vrdoljak A, O’Mahony C, Oliveira J C, Moore A C, Crean A M. Determination of parameters for successful spray coating of silicon microneedle arrays. International Journal of Pharmaceutics, 2011, 415(1): 140–149
Vrdoljak A, McGrath M G, Carey J B, Draper S J, Hill A V S, O’Mahony C, Crean A M, Moore A C. Coated microneedle arrays for transcutaneous delivery of live virus vaccines. Journal of Controlled Release, 2012, 159(1): 34–42
Gill H S, Prausnitz M R. Coated microneedles for transdermal delivery. Journal of Controlled Release, 2007, 117(2): 227–237
Chen X, Corbett H J, Yukiko S R, Raphael A P, Fairmaid E J, Prow T W, Brown L E, Fernando G J P, Kendall M A F. Site-selectively coated, densely-packed microprojection array patches for targeted delivery of vaccines to skin. Advanced Functional Materials, 2011, 21(3): 464–473
Baek S H, Shin J H, Kim Y C. Drug-coated microneedles for rapid and painless local anesthesia. Biomedical Microdevices, 2017, 19 (1): 2
Boehm R D, Miller P R, Hayes S L, Monteiro- Riviere N A, Narayan R J. Modification of microneedles using inkjet printing. AIP Advances, 2011, 1(2): 022139
Yao G, Quan G, Lin S, Peng T,Wang Q, Ran H, Chen H, Zhang Q, Wang L, Pan X, Wu C. Novel dissolving microneedles for enhanced transdermal delivery of levonorgestrel: In vitro and in vivo characterization. International Journal of Pharmaceutics, 2017, 534(1-2): 378–386
Wang C, Ye Y, Hochu G M, Sadeghifar H, Gu Z. Enhanced cancer immunotherapy by microneedle patch-assisted delivery of Anti-PD1 antibody. Nano Letters, 2016, 16(4): 2334–2340
Johnson A R, Caudill C L, Tumbleston J R, Bloomquist C J, Moga K A, Ermoshkin A, Shirvanyants D, Mecham S J, Luft J C, De Simone J M. Single-step fabrication of computationally designed microneedles by continuous liquid interface production. PLoS One, 2016, 11(9): e0162518
Caudill C L, Perry J L, Tian S, Luft J C, Desimone J M. Spatially controlled coating of continuous liquid interface production microneedles for transdermal protein delivery. Journal of Controlled Release, 2018, 284: 122–132
Chen M C, Huang S F, Lai K Y, Ling M H. Fully embeddable chitosan microneedles as a sustained release depot for intradermal vaccination. Biomaterials, 2013, 34(12): 3077–3086
Prausnitz M R, Mikszta J A, Cormier M, Andrianov A K. Microneedle-based Vaccines. Springer Berlin Heidelberg location: Springer Berlin Heidelberg, 2009, 369–393
Cheng G, Davoudi Z, Xing X, Yu X, Cheng X, Li Z, Deng H, Wang Q. Advanced silk fibroin biomaterials for cartilage regeneration. ACS Biomaterials Science & Engineering, 2018, 4 (8): 2704–2715
Zhan Y, Zeng W, Jiang G,Wang Q, Shi X, Zhou Z, Deng H, Du Y. Construction of lysozyme exfoliated rectorite-based electrospun nanofibrous membranes for bacterial inhibition. Journal of Applied Polymer Science, 2015, 132(8): 41496
Xin S, Li X,Wang Q, Huang R, Xu X, Lei Z, Deng H. Novel layerby-layer structured nanofibrous mats coated by protein films for dermal regeneration. Journal of Biomedical Nanotechnology, 2014, 10(5): 803–810