Lornoxicam controlled release transdermal gel patch: Design, characterization and optimization using co-solvents as penetration enhancers
The aim of the current study was to develop membrane-based transdermal patches of lornoxicam gel using oleic acid (OA)and propylene glycol (PG) as penetration enhancers to improve drug delivery across the skin and to evaluate in vivo analgesic and anti-inflammatory activity. For this purpose, nine f...
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| description | The aim of the current study was to develop membrane-based transdermal patches of lornoxicam gel using oleic acid (OA)and propylene glycol (PG) as penetration enhancers to improve drug delivery across the skin and to evaluate in vivo analgesic and anti-inflammatory activity. For this purpose, nine formulations were developed in accordance with 32 factorial design using Design Expert® 11. The concentration of propylene glycol (X1) and oleic acid (X2) were selected as independent variable whereas Q10 (Y1), flux (Y2) and lag time (Y3) were considered as the response variables. The impact of drug loading, surface area, gel concentration, membrane variation and agitation speed on drug release and permeation was also studied. The skin sensitivity reaction, analgesic activity and anti-inflammatory action of the optimized patch were also determined in Albino Wistar rats. Stability studies were performed for three months at three different temperature conditions. The result suggests that a membrane-based system with controlled zero-order drug release of 95.8 ± 1.121% for 10 h exhibiting flux of 126.51±1.19 μg/cm2/h and lag time of 0.908 ±0.57h was optimized with the desired analgesic and anti-inflammatory effect can be obtained by using propylene glycol and oleic acid co-solvents as a penetration enhancer. The patch was also found stable at 4˚C for a period of 6.44 months. Formulation F9 comprising of 10% PG and 3% OA was selected as an optimized formulation. The study demonstrates that the fabricated transdermal system of lornoxicam can deliver the drug through the skin in a controlled manner with desired analgesic and anti-inflammatory activity and can be considered as a suitable alternative of the oral route. |
| doi_str_mv | 10.1371/journal.pone.0228908 |
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For this purpose, nine formulations were developed in accordance with 32 factorial design using Design Expert® 11. The concentration of propylene glycol (X1) and oleic acid (X2) were selected as independent variable whereas Q10 (Y1), flux (Y2) and lag time (Y3) were considered as the response variables. The impact of drug loading, surface area, gel concentration, membrane variation and agitation speed on drug release and permeation was also studied. The skin sensitivity reaction, analgesic activity and anti-inflammatory action of the optimized patch were also determined in Albino Wistar rats. Stability studies were performed for three months at three different temperature conditions. The result suggests that a membrane-based system with controlled zero-order drug release of 95.8 ± 1.121% for 10 h exhibiting flux of 126.51±1.19 μg/cm2/h and lag time of 0.908 ±0.57h was optimized with the desired analgesic and anti-inflammatory effect can be obtained by using propylene glycol and oleic acid co-solvents as a penetration enhancer. The patch was also found stable at 4˚C for a period of 6.44 months. Formulation F9 comprising of 10% PG and 3% OA was selected as an optimized formulation. The study demonstrates that the fabricated transdermal system of lornoxicam can deliver the drug through the skin in a controlled manner with desired analgesic and anti-inflammatory activity and can be considered as a suitable alternative of the oral route.</description><identifier>ISSN: 1932-6203</identifier><identifier>EISSN: 1932-6203</identifier><identifier>DOI: 10.1371/journal.pone.0228908</identifier><identifier>PMID: 32107483</identifier><language>eng</language><publisher>United States: Public Library of Science</publisher><subject>Adhesives ; Administration, Cutaneous ; Analgesics ; Analgesics - pharmacology ; Animals ; Anti-inflammatory agents ; Anti-Inflammatory Agents, Non-Steroidal - pharmacology ; Arthritis ; Characterization ; Chemistry, Pharmaceutical ; Chronic illnesses ; Controlled release ; Delayed-Action Preparations - pharmacology ; Design ; Design optimization ; Drug delivery ; Drug delivery systems ; Drug Delivery Systems - methods ; Drug dosages ; Edema ; Factorial design ; Fatty acids ; Gels - metabolism ; Glycols (Class of compounds) ; Independent variables ; Inflammation ; Laboratory animals ; Lag time ; Male ; Medicine and Health Sciences ; Membranes ; Monounsaturated fatty acids ; Nonsteroidal anti-inflammatory drugs ; Oleic acid ; Oleic Acid - pharmacology ; Optimization ; Oral administration ; Penetration ; Pharmaceutical sciences ; Pharmacy ; Physical Sciences ; Piroxicam - analogs & derivatives ; Piroxicam - pharmacology ; Propylene ; Propylene glycol ; Propylene Glycol - pharmacology ; Rats ; Rats, Wistar ; Skin ; Skin - metabolism ; Skin Absorption - physiology ; Solvents ; Solvents - pharmacology ; Time ; Topical analgesics ; Transdermal medication ; Transdermal Patch ; Unsaturated fatty acids ; Viscosity</subject><ispartof>PloS one, 2020-02, Vol.15 (2), p.e0228908</ispartof><rights>COPYRIGHT 2020 Public Library of Science</rights><rights>2020 Hashmat et al. This is an open access article distributed under the terms of the Creative Commons Attribution License: http://creativecommons.org/licenses/by/4.0/ (the “License”), which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. 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For this purpose, nine formulations were developed in accordance with 32 factorial design using Design Expert® 11. The concentration of propylene glycol (X1) and oleic acid (X2) were selected as independent variable whereas Q10 (Y1), flux (Y2) and lag time (Y3) were considered as the response variables. The impact of drug loading, surface area, gel concentration, membrane variation and agitation speed on drug release and permeation was also studied. The skin sensitivity reaction, analgesic activity and anti-inflammatory action of the optimized patch were also determined in Albino Wistar rats. Stability studies were performed for three months at three different temperature conditions. The result suggests that a membrane-based system with controlled zero-order drug release of 95.8 ± 1.121% for 10 h exhibiting flux of 126.51±1.19 μg/cm2/h and lag time of 0.908 ±0.57h was optimized with the desired analgesic and anti-inflammatory effect can be obtained by using propylene glycol and oleic acid co-solvents as a penetration enhancer. The patch was also found stable at 4˚C for a period of 6.44 months. Formulation F9 comprising of 10% PG and 3% OA was selected as an optimized formulation. The study demonstrates that the fabricated transdermal system of lornoxicam can deliver the drug through the skin in a controlled manner with desired analgesic and anti-inflammatory activity and can be considered as a suitable alternative of the oral route.</abstract><cop>United States</cop><pub>Public Library of Science</pub><pmid>32107483</pmid><doi>10.1371/journal.pone.0228908</doi><tpages>e0228908</tpages><orcidid>https://orcid.org/0000-0002-3639-0026</orcidid><oa>free_for_read</oa></addata></record> |
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| ispartof | PloS one, 2020-02, Vol.15 (2), p.e0228908 |
| issn | 1932-6203 1932-6203 |
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| recordid | cdi_plos_journals_2366603959 |
| source | PLoS; MEDLINE; DOAJ Directory of Open Access Journals; PubMed Central; Free Full-Text Journals in Chemistry; EZB Electronic Journals Library |
| subjects | Adhesives Administration, Cutaneous Analgesics Analgesics - pharmacology Animals Anti-inflammatory agents Anti-Inflammatory Agents, Non-Steroidal - pharmacology Arthritis Characterization Chemistry, Pharmaceutical Chronic illnesses Controlled release Delayed-Action Preparations - pharmacology Design Design optimization Drug delivery Drug delivery systems Drug Delivery Systems - methods Drug dosages Edema Factorial design Fatty acids Gels - metabolism Glycols (Class of compounds) Independent variables Inflammation Laboratory animals Lag time Male Medicine and Health Sciences Membranes Monounsaturated fatty acids Nonsteroidal anti-inflammatory drugs Oleic acid Oleic Acid - pharmacology Optimization Oral administration Penetration Pharmaceutical sciences Pharmacy Physical Sciences Piroxicam - analogs & derivatives Piroxicam - pharmacology Propylene Propylene glycol Propylene Glycol - pharmacology Rats Rats, Wistar Skin Skin - metabolism Skin Absorption - physiology Solvents Solvents - pharmacology Time Topical analgesics Transdermal medication Transdermal Patch Unsaturated fatty acids Viscosity |
| title | Lornoxicam controlled release transdermal gel patch: Design, characterization and optimization using co-solvents as penetration enhancers |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-24T22%3A31%3A29IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-gale_plos_&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Lornoxicam%20controlled%20release%20transdermal%20gel%20patch:%20Design,%20characterization%20and%20optimization%20using%20co-solvents%20as%20penetration%20enhancers&rft.jtitle=PloS%20one&rft.au=Hashmat,%20Durriya&rft.date=2020-02-27&rft.volume=15&rft.issue=2&rft.spage=e0228908&rft.pages=e0228908-&rft.issn=1932-6203&rft.eissn=1932-6203&rft_id=info:doi/10.1371/journal.pone.0228908&rft_dat=%3Cgale_plos_%3EA615435107%3C/gale_plos_%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=2366603959&rft_id=info:pmid/32107483&rft_galeid=A615435107&rft_doaj_id=oai_doaj_org_article_5df0ffdb9a504638b4e2fdfeb03aefed&rfr_iscdi=true |