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Microneedle-enhanced codrug delivery for smoking cessation and appetite suppressi

Award Number: R21DA031439
ORGANIZATION: NATIONAL INSTITUTE ON DRUG ABUSE
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 07/15/2012
PERIOD OF PERFORMANCE END DATE: 06/30/2014

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Microneedle-enhanced codrug delivery for smoking cessation and appetite suppressi - DESCRIPTION (provided by applicant): Tobacco addiction is a multi-factorial process, regulated by a number of pharmacological and physiological effects of tobacco smoke exposure. In addition to the well-known effects of tobacco derived nicotine on brain dopaminergic systems, other secondary reinforcers such as body mass regulation are also involved with the compulsive tobacco use. Cigarette smoking is known to reduce appetite and increase the rate of cellular metabolism, leading to body mass stabilization or reduction. Current smoking cessation treatments fail in up to 70% of cases, for a variety of individualized reasons. One of the main reasons for recidivism, especially in females, is the potential for weight gain. The problem of weight gain during smoking cessation is well documented, and studies consistently recommend incorporation of body weight management strategies to patient management plans. The proposed studies will use a novel microneedle-enhanced transdermal codrug delivery approach to test a new pharmacological approach that we hypothesize will enhance smoking cessation efforts. Bupropion is considered a first-line treatment for smoking cessation, but the efficacy of this drug is relatively low. Hydroxybupropion (BUPOH) is an active metabolite of bupropion that may have significant drug delivery and therapeutic effect advantages over bupropion, including better chemical stability, reduced metabolic drug interaction potential, and an equal or higher potency at relevant drug targets. BUPOH itself does not have the essential physicochemical properties that would allow a therapeutic dose of the drug to cross the human skin barrier. Microneedle-enhanced transdermal delivery is an efficient and painless method for increasing the skin permeation of many drugs. The proposed studies will test whether chemical modification optimization of the BUPOH codrug will enhance its microneedle-assisted skin permeation making it suitable for transdermal delivery. Hydroxybupropion will be chemically combined with phentermine (PHEN), a widely used appetite suppressant. PHEN should have a more tolerable side-effect profile if delivered at a constant rate through transdermal delivery. We hypothesize that a transdermal codrug (mutual prodrug or hybrid drug) of PHEN linked to the smoking cessation drug, BUPOH, will make an effective microneedle-enhanced transdermal pharmacotherapy for smoking cessation and weight loss. The specific aims of this project are to: 1 - synthesize a series of PHEN and BUPOH codrugs designed to elucidate quantitative structure-permeability relationships (QSPR) for microneedle-enhanced transdermal flux and subsequent bioconversion rates. 2 - to measure the drugs' penetration and concurrent bioconversion in skin in vitro with microneedle use, and 3 - to characterize the pharmacokinetics of the drugs in guinea pigs in vivo with microneedle use. Correlation of our in vitro data with the in vivo model will aid in the creation of a reliable QSPR database for transdermal codrugs with microneedle use, as well as help to identify the most promising codrug/microneedle system for eventual human use.


Issue Date FY	Funding FY	Legal Entity Name	Legal Entity Address	Legal Entity City	Legal Entity State	Legal Entity Zip Code	Legal Entity COUNTY	Legal Entity COUNTRY	Assistance Listing	Award Code	Budget Year	Action Date	Action Type	Action Amount

Issue Date FY: 2017 ( Subtotal = -$17,709 )
2017	2013	ZYNERBA PHARMACEUTICALS, INC.	80 W LANCASTER AVE SUITE 300	DEVON	PA	19333	CHESTER	USA	Drug Use and Addiction Research Programs	000	2	1/9/2017	NON-COMPETING CONTINUATION	-$17,709
														Subtotal = -$17,709

Issue Date FY: 2015 ( Subtotal = $0 )
2015	2013	ALLTRANZ INC	4080 WEBER WAY	LEXINGTON	KY	40514	FAYETTE	USA	Drug Use and Addiction Research Programs	000	2	10/31/2014	NON-COMPETING CONTINUATION	$0
														Subtotal = $0

Issue Date FY: 2013 ( Subtotal = $230,144 )
2013	2013	ALLTRANZ INC	4080 WEBER WAY	LEXINGTON	KY	40514	FAYETTE	USA	Drug Use and Addiction Research Programs	000	2	4/16/2013	NON-COMPETING CONTINUATION	$215,760
2013	2013	ALLTRANZ INC	4080 WEBER WAY	LEXINGTON	KY	40514	FAYETTE	USA	Drug Use and Addiction Research Programs	001	2	5/16/2013	NON-COMPETING CONTINUATION	$14,384
														Subtotal = $230,144

Issue Date FY: 2012 ( Subtotal = $203,625 )
2012	2012	ALLTRANZ INC	4080 WEBER WAY	LEXINGTON	KY	40514	FAYETTE	USA	Drug Use and Addiction Research Programs	000	1	7/11/2012	NEW	$203,625
														Subtotal = $203,625

Grand Total All Awards = $416,060

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Microneedle-enhanced codrug delivery for smoking cessation and appetite suppressi

Award Number: R21DA031439

ORGANIZATION: NATIONAL INSTITUTE ON DRUG ABUSE

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)

PERIOD OF PERFORMANCE START DATE: 07/15/2012

PERIOD OF PERFORMANCE END DATE: 06/30/2014

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