Deep Percutaneous Penetration into Muscles and Joints: Update
Keywords:
topical administration, non-steroidal anti-inflammatory agents, skin absorption, percutaneous drug deliveryAbstract
Transdermal drug delivery is a multifactorial process with variable penetration mechanisms. Adverse effects associated with nonsteroidal anti-inflammatory drugsÊ (NSAIDs) use in treatment for joint and muscle diseases are sufficiently severe to consider topical application. A drug's lipophilicity, fraction unbound and permeability found in the viable skin are some of the physiochemical factors influencing the delivery mechanism of transdermal absorption. These and other variables play a role in determining if the drug reaches the deep tissues via direct penetration from dermal or systemic blood redistribution. Pharmacokinetic models have been developed to help elucidate penetration routes and efficacy for various drugs. Improvements in modes of transdermal delivery through active research projects including relevant animal models and human translational research may introduce advances in clinical development of treatments.
References
. Prieto-Alhambra D, Judge A, Javaid MK, Cooper C, Diez-Perez A, Arden NK. Incidence and risk factors for clinically diagnosed knee, hip and hand osteoarthritis: influences of age, gender and osteoarthritis affecting other joints. Ann Rheum Dis 2013. doi:10.1136/annrheumdis-2013-203355
. Singh P. Percutaneous penetration as a method of delivery to skin and underlying tissues. In: Bronaugh RL, Maibach HI, editors. Percutaneous Absorption: Drugs-Cosmetics-MEchanisms-Methodology. 7th ed. New York: Marcel Dekker Inc.; 1999. p. 597-613.
. Guy RH. Transdermal drug delivery. In: Schafer-Korting M, editor. Drug Delivery. 197th ed. Vol. 197. Springer; 2010. p. 399–410.
. Stanos S P. Osteoarthritis guidelines: a progressive role for topical nonsteroidal anti-inflammatory drugs. Journal of multidisciplinary healthcare. 2013; 6:133–7.
. Lee CM, Maibach HI. Deep percutaneous penetration into muscles and joints. Journal of pharmaceutical sciences, 2006; 95(7): 1405–13.
. Jepps OG, Dancik Y, Anissimov YG, Roberts MS. Modeling the human skin barrier--towards a better understanding of dermal absorption. Advanced drug delivery reviews. 2013;65(2): 152–68.
. Singh P, Roberts MS. Skin permeability and local tissue concentrations of nonsteroidal anti-inflammatory drugs after topical application. The Journal of pharmacology and experimental therapeutics. 1994a; 268(1): 144–51.
. Singh P, Roberts MS. Deep tissue penetration of bases and steroids after dermal application in rat. The Journal of pharmacy and pharmacology.1994b; 46(12): 956–64.
. Baldwin JR, Carrano R A, Imondi AR. Penetration of trolamine salicylate into the skeletal muscle of the pig. Journal of pharmaceutical sciences. 1984; 73(7): 1002–4.
. Herndon C M. Topical delivery of nonsteroidal anti-inflammatory drugs for osteoarthritis. Journal of pain & palliative care pharmacotherapy. 2012; 26(1): 18–23.
. Roberts MS, Anderson RA, Swarbrick J. Permeability of human epidermis to phenolic compounds. The Journal of pharmacy and pharmacology.1977; 29(11): 677–83.
. Swarbrick J, Lee G, Brom J, Gensmantel N P. Drug permeation through human skin II: Permeability of ionizable compounds. Journal of pharmaceutical sciences.1984; 73(10): 1352–5.
. Magnusson BM, Anissimov Y G, Cross SE, Roberts MS. Molecular size as the main determinant of solute maximum flux across the skin. The Journal of investigative dermatology. 2004; 122(4): 993–9.
. Higaki K, Asai M, Suyama T, Nakayama K, Ogawara K, Kimura T. Estimation of intradermal disposition kinetics of drugs: II. Factors determining penetration of drugs from viable skin to muscular layer. International journal of pharmaceutics. 2002;239(1-2): 129–41
. Yagi S, Nakayama K, Kurosaki Y, Higaki K, Kimura T. Factors determining drug residence in skin during transdermal absorption: studies on beta-blocking agents. Biological & pharmaceutical bulletin.1998; 21(11): 1195–201.
. Guy RH, Hadgraft J, Maibach HI. A pharmacokinetic model for percutaneous absorption. International Journal of Pharmaceutics.1982; 11(2): 119–129.
. Barry B. Transdermal drug delivery. In: Aulton M, editor. Pharmaceutics: the science of dosage form design. London: Harcourt Publishers Ltd.; 1988. p. 499–533.
. Higaki K, Nakayama K, Suyama T, Amnuaikit C, Ogawara K, Kimura, T. Enhancement of topical delivery of drugs via direct penetration by reducing blood flow rate in skin. International journal of pharmaceutics.2005; 288(2): 227–33.
. Singh P, Roberts MS. Dermal and underlying tissue pharmacokinetics of salicylic acid after topical application. Journal of pharmacokinetics and biopharmaceutics.1993a; 21(4): 337–73.
. Singh P, Roberts MS. Iontophoretic transdermal delivery of salicylic acid and lidocaine to local subcutaneous structures. Journal of pharmaceutical sciences. 1993b;82(2): 127–31.
. Kretsos K, Kasting GB, Nitsche JM. Distributed diffusion-clearance model for transient drug distribution within the skin. Journal of pharmaceutical sciences. 2004;93(11): 2820–35.
. Kretsos K, Kasting GB. A geometrical model of dermal capillary clearance. Mathematical biosciences.2007; 208(2): 430–53.
. Schaefer H, Stüttgen G. Absolute concentrations of an antimycotic agent, econazole, in the human skin after local application. Arzneimittel-Forschung. 1976;26(3): 432–5.
. Schaefer H, Zesch A. Penetration of vitamin A acid into human skin. Acta dermato-venereologica. Supplementum. 1975; 74: 50–5.
. Zesch A, Schaefer H. [Penetration of radioactive hydrocortisone in human skin from various ointment bases. II. In vivo-experiments (author’s transl)]. Archiv für dermatologische Forschung; 1975;252(4): 245–56.
. Schaefer H, Zesch A, Stüttgen G. Penetration, permeation, and absorption of triamcinolone acetonide in normal and psoriatic skin. Archives for dermatological research. Archiv für dermatologische Forschung.1977; 258(3): 241–9.
. Schaefer H, Stüttgen G, Zesch A, Schalla W, Gazith J. Quantitative determination of percutaneous absorption of radiolabeled drugs in vitro and in vivo by human skin. Current problems in dermatology.1978; 7:80–94.
. Anissimov YG, Roberts MS. Modelling dermal drug distribution after topical application in human. Pharmaceutical research.2011; 28(9):2119–29.
. Dancik Y, Anissimov YG, Jepps O G, Roberts MS. Convective transport of highly plasma protein bound drugs facilitates direct penetration into deep tissues after topical application. British journal of clinical pharmacology.2012; 73(4): 564–78.
. Yanagimoto G, Hayashi T, Hasegawa T, Seki T, Juni K, Sugibayashi K, Morimoto Y. Skin disposition of drugs after topical application in hairless rats. Chemical & pharmaceutical bulletin.1999; 47(6): 749–54.
. Radermacher J, Jentsch D, Scholl M A, Lustinetz T, Frölich J C. Diclofenac concentrations in synovial fluid and plasma after cutaneous application in inflammatory and degenerative joint disease. British journal of clinical pharmacology.1991; 31(5): 537–41.
. Müller M, Rastelli C, Ferri P, Jansen B, Breiteneder H, Eichler HG. Transdermal penetration of diclofenac after multiple epicutaneous administration. The Journal of rheumatology.1998;25(9): 1833–6.
. Miyatake S, Ichiyama H, Kondo E, Yasuda K. Randomized clinical comparisons of diclofenac concentration in the soft tissues and blood plasma between topical and oral applications. British journal of clinical pharmacology.2009; 67(1): 125–9.
. Kai S, Kondo E, Kawaguchi Y, Kitamura N, Yasuda K. Flurbiprofen concentration in soft tissues is higher after topical application than after oral administration. British journal of clinical pharmacology.2013; 75(3): 799–804.
. Rabinowitz JL, Baker D. Absorption of labeled triethanolamine salicylate in human and canine knee joints. II. Journal of clinical pharmacology.1984;24(11-12): 532–9.
. Mills PC, Magnusson BM, Cross SE. Penetration of a topically applied nonsteroidal anti-inflammatory drug into local tissues and synovial fluid of dogs. American journal of veterinary research. 2005;66(7):1128–32.
. Yoshida D, Hasegawa T, Sugibayashi K.Targeting of salicylate to skin and muscle following topical injections in rats. International journal of pharmaceutics. 2002; 231(2): 177–84.
. Skazik C, Wenzel J, Marquardt Y, Kim A, Merk HF, Bickers DR, Baron JM(2011). P-glycoprotein (ABCB1) expression in human skin is mainly restricted to dermal components. Experimental dermatology. 2011; 20(5): 450–2.
. Polat BE, Hart D, Langer R, Blankschtein D. Ultrasound-mediated transdermal drug delivery: mechanisms, scope, and emerging trends. Journal of controlled release : official journal of the Controlled Release Society.2011; 152(3): 330–48.
. Kigasawa K, Kajimoto K, Watanabe M, Kanamura K, Saito A, Kogure K. In vivo transdermal delivery of diclofenac by ion-exchange iontophoresis with geraniol. Biological & pharmaceutical bulletin.2009;32(4): 684–7.
. Sammeta SM, Murthy SN. “ChilDrive”: a technique of combining regional cutaneous hypothermia with iontophoresis for the delivery of drugs to synovial fluid. Pharmaceutical research.2009; 26(11): 2535–40.
. Tugwell PS, Wells GA, Shainhouse JZ. Equivalence study of a topical diclofenac solution (pennsaid) compared with oral diclofenac in symptomatic treatment of osteoarthritis of the knee: a randomized controlled trial. The Journal of rheumatology.2004; 31(10):2002–12.
. Simon LS, Grierson LM, Naseer Z, Bookman AAM, Zev Shainhouse J. Efficacy and safety of topical diclofenac containing dimethyl sulfoxide (DMSO) compared with those of topical placebo, DMSO vehicle and oral diclofenac for knee osteoarthritis. Pain. 2009;143(3):238–45.
. Roth SH, Fuller P. Diclofenac topical solution compared with oral diclofenac: a pooled safety analysis. Journal of pain research.2011; 4: 159–67.
. Bookman AAM, Williams KSA, Shainhouse JZ. Effect of a topical diclofenac solution for relieving symptoms of primary osteoarthritis of the knee: a randomized controlled trial. Canadian Medical Association journal.2004; 171(4): 333–8.
. Carnes D, Anwer Y, Underwood M, Harding G, Parsons S. Influences on older people’s decision making regarding choice of topical or oral NSAIDs for knee pain: qualitative study. BMJ.2008;336(7636): 142–5.
. Makris UE, Kohler MJ, Fraenkel L. Adverse effects of topical nonsteroidal antiinflammatory drugs in older adults with osteoarthritis: a systematic literature review. The Journal of rheumatology.2010; 37(6): 1236–43.
. Haisch C. Photoacoustic spectroscopy for analytical measurements. Measurement Science and Technology. 2012; 23.
. De Melo JO, Pedrochi F, Baesso ML, Hernandes L, Truiti MCT, Barons S, Bersani-Amado CA. Evidence of deep percutaneous penetration associated with anti-inflammatory activity of topically applied Helicteres gardneriana extract: a photoacoustic spectroscopy study. Pharmaceutical research. 2011; 28(2): 331–6.
. Xi H, Cun D, Xiang R, Guan Y, Zhang Y, Li Y, Fang L.Intra-articular drug delivery from an optimized topical patch containing teriflunomide and lornoxicam for rheumatoid arthritis treatment: Does the topical patch really enhance a local treatment? Journal of controlled release : official journal of the Controlled Release Society.2013; 169(1-2):73–81.
