title: Innovative polymeric system (IPS) for solvent-free lipophilic drug transdermal delivery via dissolving microneedles.
abstract: Lipophilic drugs are potential drug candidates during drug development. However, due to the need for hazardous organic solvents for their solubilization, these drugs often fail to reach the pharmaceutical market, and in doing so highlight the importance of solvent free systems. Although transdermal drug delivery systems (TDDSs) are considered prospective safe drug delivery routes, a system involving lipophilic drugs in solvent free or powder form has not yet been described. Here, we report, for the first time, a novel approach for the delivery of every kind of lipophilic drug in powder form based on an innovative polymeric system (IPS). The phase transition of powder form of lipophilic drugs due to interior chemical bonds between drugs and biodegradable polymers and formation of nano-sized colloidal structures allowed the fabrication of dissolving microneedles (DMNs) to generate a powerful TDDS. We showed that IPS based DMN with powder capsaicin enhances the therapeutic effect for treatment of the rheumatic arthritis in a DBA/1 mouse model compared to a solvent-based system, indicating the promising potential of this new solvent-free platform for lipophilic drug delivery.
authors.affiliation: Department of Biotechnology, Building 123, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea.
authors.forename: Manita
authors.initials: M
authors.lastname: Dangol
authors.affiliation: Department of Biotechnology, Building 123, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea.
authors.forename: Huisuk
authors.initials: H
authors.lastname: Yang
authors.affiliation: Department of Biotechnology, Building 123, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea.
authors.forename: Cheng Guo
authors.initials: CG
authors.lastname: Li
authors.affiliation: Department of Biotechnology, Building 123, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea.
authors.forename: Shayan Fakhraei
authors.initials: SF
authors.lastname: Lahiji
authors.affiliation: Department of Biotechnology, Building 123, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea.
authors.forename: Suyong
authors.initials: S
authors.lastname: Kim
authors.affiliation: Department of Biotechnology, Building 123, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea.
authors.forename: Yonghao
authors.initials: Y
authors.lastname: Ma
authors.affiliation: Department of Biotechnology, Building 123, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea; Juvic Biotech. Inc., Building 102, Yonsei Engineering Research Park, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea. Electronic address: hijung@yonsei.ac.kr.
authors.forename: Hyungil
authors.initials: H
authors.lastname: Jung
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D001172:Arthritis, Rheumatoid / Q000139:chemically induced / Q000188:drug therapy* / Q000473:pathology; D002211:Capsaicin / Q000008:administration & dosage* / Q000737:chemistry / Q000627:therapeutic use; D024043:Collagen Type II; D016503:Drug Delivery Systems; D065546:Drug Liberation; D005260:Female; D008811:Mice, Inbred DBA; D008845:Microinjections; D009339:Needles; D010316:Particle Size; D011142:Polyvinyl Alcohol / Q000737:chemistry; D011205:Povidone / Q000737:chemistry; D011208:Powders; D012995:Solubility
chemical_list: D024043:Collagen Type II; D011208:Powders; D011142:Polyvinyl Alcohol; D011205:Povidone; D002211:Capsaicin
keywords: Colloids; Dissolving microneedle; Lipophilic drugs; Rheumatic arthritis; Solvent free system; Transdermal drug delivery