Cannabidiol bioavailability after nasal and transdermal application: Effect of permeation enhancers

Drug Development and Industrial Pharmacy

Volumn 36, Issue 9, 2010, Pages 1088-1097

  Paudel, Kalpana S ^a   Hammell, Dana C ^a,b   Agu, Remigius U ^a   Valiveti, Satyanarayana ^a   Stinchcomb, Audra L ^a,b  

^a University of Kentucky   (United States)

^b AllTranz Inc   (United States)

Author keywords

Cannabidiol; Cannabinoids; Guinea pig; In vitro studies; In vivo studies; Intranasal; Pharmacokinetics; Rat; Transdermal

Indexed keywords

CANNABIDIOL; MACROGOL; PENETRATION ENHANCING AGENT;

ANIMAL MODEL; ARTICLE; CHRONIC PAIN; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG DELIVERY SYSTEM; FEMALE; GUINEA PIG; IN VITRO STUDY; IN VIVO STUDY; MALE; NONHUMAN; RAT; STEADY STATE;

ABSORPTION; ADMINISTRATION, CUTANEOUS; ADMINISTRATION, INTRANASAL; ANALGESICS; ANIMALS; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CANNABIDIOL; CANNABINOIDS; DRUG COMPOUNDING; DRUG DELIVERY SYSTEMS; EXCIPIENTS; FEMALE; GUINEA PIGS; MALE; PERMEABILITY; RATS; RATS, HAIRLESS; SKIN;

EID: 77956418173     PISSN: 03639045     EISSN: 15205762     Source Type: Journal    
DOI: 10.3109/03639041003657295     Document Type: Article

References (42)

1. Parker LA, Mechoulam R, Schlievert C. (2002). Cannabidiol, a non-psychoactive component of cannabis and its synthetic dimethylheptyl homolog suppress nausea in an experimental model with rats. NeuroReport, 13:567-70.
2. Costa B, Colleoni M, Conti S, Parolaro D, Franke C, Trovato AE, et al. (2004). Oral anti-inflammatory activity of cannabidiol, a non-psychoactive constituent of cannabis, in acute carrageenan- induced inflammation in the rat paw. Naunyn Schmiedebergs Arch Pharmacol, 369:294-9.
3. Holdcroft A, Maze M, Doré C, Tebbs S, Thompson S. (2006). A multicenter dose-escalation study of the analgesic and adverse effects of an oral cannabis extract (Cannador) for postoperative pain management. Anesthesiology, 104:1040-6.
4. Zajicek J, Fox P, Sanders H, Wright D, Vickery J, Nunn A, et al. (2003). Cannabinoids for treatment of spasticity and other symptoms related to multiple sclerosis (CAMS study): Multicentre randomised placebo-controlled trial. Lancet, 362:1517-26.
5. Rog DJ, Nurmikko TJ, Friede T, Young CA. (2005). Randomized, controlled trial of cannabis-based medicine in central pain in multiple sclerosis. Neurology, 65:812-9.
6. Blake DR, Robson P, Ho M, Jubb RW, McCabe CS. (2006). Preliminary assessment of the efficacy, tolerability and safety of a cannabis-based medicine (Sativex) in the treatment of pain caused by rheumatoid arthritis. Rheumatology, 45:50-2.
7. Agurell S, Carlsson S, Lindgren JE, Ohlsson A, Gillspie H, Hollister L. (1981). Interaction of THC with cannabinol and cannabidiol following oral administration in man. Assay of cannabinol and cannabidiol by mass fragmentography. Experientia, 37:1090-2.
8. Ohisson A, Lindgren JE, Andersson S, Agurell S, Gillespie H, Hollister LE. (1986). Single-dose kinetics of deutrium-labeled cannabidiol in man after smoking and intravenous administration. Biomed Environ Mass Spectrom, 13:77-83.
9. Samara E, Bialer M, Mechoulam R. (1988). Pharmacokinetics of cannabidiol in dogs. Drug Metab Dispos, 16:469-72.
10. Holdcroft A, Smith M, Smith B, Hodgson H, Evans FJ. (1997). Clinical trial experience with cannabinoids. Pharm Sci, 3:546-50.
11. Welch SP, Eads M. (1999). Synergistic interactions of endogenous opioids and cannabinoid systems. Brain Res, 848:183-90.
12. Cichewicz DL, McCarthy EA. (2003). Antinociceptive synergy between Ä9-tetrahydrocannabinol and opioids after oral administration. JPET, 304:1010-5.
13. Touitou E, Fabin B, Dany S, Almog S. (1988). Transdermal delivery of tetrahydrocannabinol. Int J Pharm, 43:9-15.
14. Touitou E, Fabin B. (1988). Altered skin permeation of a highly lipophilic molecule: Tetrahydrocannabinol. Int J Pharm, 43:17-22.
15. Fabin B, Touitou E. (1991). Localization of lipophilic molecules penetrating rat skin in vivo by quantitative autoradiography. Int J Pharm, 74:59-65.
16. Challapalli PV, Stinchcomb AL. (2002). In vitro experiment optimization for measuring tetrahydrocannabinol skin permeation. Int J Pharm, 241:329-39.
17. Valiveti S, Hammell DC, Earles DC, Stinchcomb AL. (2004a). In vitro/in vivo correlation studies for transdermal delta 8-THC development. J Pharm Sci, 93:1154-64. (Pubitemid 38529689)
18. Valiveti S, Hammell DC, Earles DC, Stinchcomb AL. (2004b). Transdermal delivery of the synthetic cannabinoid WIN 55212- 2: In vitro/in vivo correlation. Pharm Res, 21:1137-45.
19. Valiveti S, Kiptoo PK, Hammell DC, Stinchcomb AL. (2004). Transdermal permeation of WIN 55212-2 and CP 55940 in human skin in vitro. Int J Pharm, 278:173-80.
20. Stinchcomb AL, Valiveti S, Hammell DC, Ramsey DR. (2004). Human skin permeation of Delta8-tetrahydrocannabinol, cannabidiol and cannabinol. J Pharm Pharmacol, 56:291-7. (Pubitemid 38380210)
21. Lodzkia M, Godina B, Rakoua L, Mechoulamb R, Gallilyc R, Touitou E. (2003). Cannabidiol-transdermal delivery and anti-inflammatory effect in a murine model. J Control Release, 93:377-87.
22. Stinchcomb AL, Nalluri BN. (2005). Transdermal delivery of cannabinoids. US patent no. 20050266061.
23. Agu RU, Valiveti S, Paudel KS, Klausner M, Hayden PJ, Stinchcomb AL. (2006). Permeation of WIN 55212-2, a potent cannabinoid receptor agonist, across human tracheo-bronchial tissue in vitro and rat nasal epithelium in vivo. J Pharm Pharmacol, 58:1459-65.
24. Valiveti S, Agu RU, Hammell DC, Paudel KS, Earles DC, Wermeling DP, et al. (2007). Intranasal absorption of Ä9-tetrahydrocannabinol and WIN 55212-2 mesylate in rats. Eur J Pharm Biopharm, 65:247-52
25. Hussain AA, Dittert LW, Qaisi AM, Traboulsi A. (2002). Method for enhancement of delivery of THC by the administration of its prodrugs via the nasal route. US patent no. 6,380,175.
26. Hussain AA, Dakkuri A, Itoh S. (2000). Nasal absorption of ondansetron in rats: An alternative route of drug delivery. Cancer Chemother Pharmacol, 45:432-4.
27. Bagger MA, Nielsen HW, Bechgaard E. (2001). Nasal bioavailability of peptide T in rabbits: Absorption enhancement by sodium glycocholate and glycofurol. Eur J Pharm Sci, 14:69-74.
28. Li L, Gorukanti S, Choi YM, Kim KH. (2000). Rapid-onset intranasal delivery of anticonvulsants: Pharmacokinetic and pharmacodynamic evaluation in rabbits. Int J Pharm, 199:65-76.
29. Hirai S, Yashiki T, Mima H. (1981). Mechanisms for the enhancement of the nasal absorption of insulin by surfactants. Int J Pharm, 9:173-84. (Pubitemid 11021848)
30. Huang Y, Donovan MD. (1998). Large molecule and particulate uptake in the nasal cavity: The effect of size on nasal absorption. Adv Drug Deliv Rev, 29:147-55.
31. Merkus FW, Verhoef JC, Marttin E, Romeijn SG, van der Kuy PH, Hermens WA, et al. (1999). Cyclodextrins in nasal drug delivery. Adv Drug Deliv Rev, 36:41-57.
32. Marttin E, Verhoef JC, Merkus FW. (1998). Efficacy, safety and mechanism of cyclodextrins as absorption enhancers in nasal delivery of peptide and protein drugs. J Drug Target, 6:17-36.
33. Hjortkjár RK, Bechgaard E, Gizurarson SR, Suzdak C, Mcdonald P, Greenough RJ. (1999). Single- and repeated-dose local toxicity in the nasal cavity of rabbits after intranasal administration of different glycols for formulations containing benzodiazepines. J Pharm Pharmacol, 51:377-83.
34. Rahman M, Lau-Cam CA. (1999). Evaluation of the effect of polyethylene glycol 400 on the nasal absorption of nicardipine and verapamil in the rat. Pharmazie, 54:132-6.
35. Barthélémy P, Farah N, Laforet JP. (1995). Transcutol-product profile product information. Gattefossé, 1-10.
36. Yazdanian M, Chen E. (1995). The effect of diethylene glycol monoethyl ether as a vehicle for topical delivery of ivermectin. Vet Res Comm, 19:309-19.
37. Mura P, Faucci MT, Bramanti G, Corti P. (2000). Evaluation of transcutol as a clonazepam transdermal permeation enhancer from hydrophilic gel formulations. Eur J Pharm Sci, 9:365-72.
38. Cho YA, Gwak HS. (2004). Transdermal delivery of ketorolac tromethamine: Effects of vehicles and penetration enhancers. Drug Dev Ind Pharm, 30:557-64.
39. Ganem-Quintanar A, Lafforgue C, Falson-Rieg F, Buri P. (1997). Evaluation of the transepidermal permeation of diethyleneglycol monoethylether and skin water loss. Int J Pharm, 147:165-72.
40. Touitou E, Levi-Schaffer F, Dayan N, Alhaique F, Riccieri F. (1994). Modulation of caffeine skin delivery by carrier design: Liposomes versus permeation enhancers. Int J Pharm, 103:131-6.
41. Weiner B, ed. (1996). Physicians desk reference generics. New Jersey: Medical Economics, 1083-6.
42. Consroe P, Kennedy K, Schram K. (1991). Assay of plasma cannabidiol by capillary gas chromatography/ion trap mass spectroscopy following high-dose repeated daily oral administration in humans. Pharmacol Biochem Behav, 40:517-22.l