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Assignees
MemberLibero PharmaLibero PharmaLibero Pharma develops transdermal delivery systems for established opioid receptor antagonists, primarily focusing on Naltrexone, to address high unmet medical needs in chronic conditions including addiction, fibromyalgia, and Crohn’s disease. By employing patient-friendly transdermal patches, the company aims to enable better therapeutic outcomes through sustained drug delivery for individuals where existing oral or injectable treatments offer limited access or efficacy. The company has received notable research support, including a significant grant from the National Institute of Drug Abuse (NIDA), and focuses on expedited regulatory pathways leveraging established safety and efficacy data.
Libero Pharma develops transdermal delivery systems for established opioid receptor antagonists, primarily focusing on Naltrexone, to address high unmet medical needs in chronic conditions including addiction, fibromyalgia, and Crohn’s disease. By employing patient-friendly transdermal patches, the company aims to enable better therapeutic outcomes through sustained drug delivery for individuals where existing oral or injectable treatments offer limited access or efficacy. The company has received notable research support, including a significant grant from the National Institute of Drug Abuse (NIDA), and focuses on expedited regulatory pathways leveraging established safety and efficacy data.
Publication Number
US-10729686-B2
Publication Date
2020-08-04
Expiration Date
Abstract
The invention provides transdermal patches comprising an adhesive and a composition comprising naltrexone and methyl oleate or isopropyl myristate, a kit comprising a plurality of such transdermal patches, a composition comprising naltrexone and methyl oleate, such a composition for use as a medicament, and compositions comprising naltrexone and methyl oleate or isopropyl myristate for use in the treatment of alcoholism or opiate addiction.
Core Innovation
The invention relates to a transdermal patch that includes a carrier layer in which a composition comprising naltrexone and isopropyl myristate is dissolved or dispersed, an adhesive layer, and a naltrexone-permeable membrane layer positioned between and in direct physical contact with the carrier layer and the adhesive layer to separate the carrier layer from the adhesive layer. The patch is formulated for treatment of a human patient suffering from opiate addiction and is described in connection with transdermal delivery of naltrexone.
The transdermal patch delivery is further described in terms of pharmaceutical compositions and transdermal patch delivery of naltrexone using methyl oleate and/or isopropyl myristate as penetration/permeation enhancers. Different patch formats are described, including a fluid reservoir patch, a solid reservoir patch, and a monolithic patch. The described relationship between enhancer identity and adhesive properties uses an adhesive Hildebrand solubility parameter, and diffusion behavior is reported as a lag/steady-state across patch types.
The document also describes the use of in vitro Franz diffusion flux across human cadaver epidermis and reports enhanced naltrexone permeation that depends on the enhancer identity and the adhesive Hildebrand solubility parameter. Temperature effects are described in which patch/skin temperature is increased, and changes in in vitro flux are reported. Kit embodiments are described that contain multiple patches, optionally including a heat-generating system for elevating the temperature of the composition.
Claims Coverage
The document provides coverage through three independent claims: a transdermal patch claim directed to opiate addiction, and two method-of-treatment claims directed to alcoholism and opiate addiction. Across these independent claims, the main inventive features are centered on a specific patch architecture with a naltrexone/isopropyl myristate carrier composition separated from an adhesive layer by a naltrexone-permeable membrane, used to effect transdermal delivery of naltrexone to a human patient for the stated condition.
Carrier layer with naltrexone and isopropyl myristate composition
A carrier layer in which a composition comprising naltrexone and isopropyl myristate is dissolved or dispersed.
Adhesive layer
An adhesive layer.
Naltrexone-permeable membrane layer in direct contact separating carrier from adhesive
A naltrexone-permeable membrane layer between and in direct physical contact with the carrier layer and the adhesive layer to separate the carrier layer from the adhesive layer.
Formulated for treatment of a human patient suffering from opiate addiction
The transdermal patch is formulated for treatment of a human patient suffering from opiate addiction.
Affixing transdermal patch to skin to effect transdermal delivery of naltrexone
Affixing a transdermal patch to the skin of the human patient suffering from alcoholism whereby to effect transdermal delivery of naltrexone.
Formulated for treatment of alcohol addiction
The transdermal patch is formulated for treatment of alcohol addiction.
Affixing transdermal patch to skin to effect transdermal delivery of naltrexone
Affixing a transdermal patch to the skin of the human patient suffering from opiate addiction whereby to effect transdermal delivery of naltrexone.
Formulated for treatment of opiate addiction
The transdermal patch is formulated for treatment of opiate addiction.
Overall claim coverage ties the transdermal patch architecture (carrier layer containing naltrexone and isopropyl myristate, adhesive layer, and a naltrexone-permeable membrane layer in direct contact separating carrier and adhesive) to transdermal delivery of naltrexone for opiate addiction and alcoholism, with the method claims grounded in affixing the patch to skin.
Stated Advantages
Enhanced naltrexone permeation in in vitro Franz diffusion flux experiments.
Dependence of naltrexone permeation on enhancer identity and adhesive Hildebrand solubility parameter.
Temperature effects are described, including increased patch/skin temperature and associated changes in flux behavior.
Documented Applications
Treatment of a human patient suffering from opiate addiction using a transdermal patch formulated for opiate addiction.
Treatment of a human patient suffering from alcoholism using a transdermal patch formulated for alcohol addiction.
Kit embodiments containing multiple transdermal patches for the described delivery and treatment context.
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