title: Development of DH-I-180-3 loaded lipid nanoparticle for photodynamic therapy.
abstract: Photodynamic therapy (PDT) is a promising noninvasive treatment modality for cancer. Photosensitizer and specific wave length of light are the key component of PDT. DH-I-180-3, a second generation photosensitizer, was incorporated into lipid nanoparticle for simultaneous fluorescent imaging and targeting therapy. Solid lipid nanoparticle (SLN) and nanostructured lipid carriers (NLC) based on poloxamer 188 as surfactant and lecithin as co-surfactant were prepared using solvent evaporation and hot homogenization technique. Stearic acid and Capmul(®) MCM C8 were utilized as solid lipid and liquid lipid, respectively. The particle size of SLN and NLCs was around 200 nm and decreased when a part of stearic acid was replaced with Capmul(®) MCM C8. Drug loading efficacy was significantly enhanced when the percentage amount of liquid lipid increased. All the polydispersity indices of the SLN/NLCs were below 0.3, and displayed a narrow particle size distribution. Zeta potentials of all the lipid nanoparticles were below -30 mV, maintaining sufficient repulsive force and achieving enhanced physical stability. No significant change in the particle size and polydispersity index was observed from lyophilized SLN/NLCs. When the photocytotoxic effects of the formulations were evaluated in MCF-7 cells, GI 50 of SLN was less than half of DH-I-180-3 solution, and NLCs containing either 5 or 15%w/w of Capmul(®) MCM C8 exerted higher cytotoxicity than SLN. The fluorescence microscope images displayed enhanced cellular accumulation of DH-I-180-3 loaded in SLN and NLCs, which was closely correlated with the photocytotoxicity results. It was concluded that the incorporation of DH-I-180-3 into the nanoparticles enhanced their targeting efficacy and improved photocytotoxicity.
authors.affiliation: College of Pharmacy, Chosun University, Gwangju, Republic of Korea.
authors.forename: Jun-Hyung
authors.initials: JH
authors.lastname: Park
authors.affiliation: College of Pharmacy, Chosun University, Gwangju, Republic of Korea.
authors.forename: Sang-Jun
authors.initials: SJ
authors.lastname: Ban
authors.affiliation: College of Pharmacy, Chosun University, Gwangju, Republic of Korea.
authors.forename: Taksim
authors.initials: T
authors.lastname: Ahmed
authors.affiliation: College of Pharmacy, Chosun University, Gwangju, Republic of Korea.
authors.forename: Hong Seok
authors.initials: HS
authors.lastname: Choi
authors.affiliation: Department of Oral and Maxillofacial Pathology, Daejeon Dental Hospital, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Wonkwang University, Daejeon, Republic of Korea.
authors.forename: Hyo-Eun
authors.initials: HE
authors.lastname: Yoon
authors.affiliation: Department of Oral and Maxillofacial Pathology, Daejeon Dental Hospital, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Wonkwang University, Daejeon, Republic of Korea.
authors.forename: Jung-Hoon
authors.initials: JH
authors.lastname: Yoon
authors.affiliation: College of Pharmacy, Chosun University, Gwangju, Republic of Korea. Electronic address: hgchoi@chosun.ac.kr.
authors.forename: Hoo-Kyun
authors.initials: HK
authors.lastname: Choi
mesh_terms: D002210:Caprylates; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D002734:Chlorophyll / Q000008:administration & dosage / Q000031:analogs & derivatives*; D004337:Drug Carriers; D005989:Glycerides; D006801:Humans; D054709:Lecithins; D008055:Lipids / Q000737:chemistry*; D061986:MCF-7 Cells; D053758:Nanoparticles / Q000008:administration & dosage; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000008:administration & dosage*; D020442:Poloxamer; D013229:Stearic Acids; D013501:Surface-Active Agents
chemical_list: D002210:Caprylates; C000607508:DH-I-180-3; D004337:Drug Carriers; D005989:Glycerides; D054709:Lecithins; D008055:Lipids; D017319:Photosensitizing Agents; D013229:Stearic Acids; D013501:Surface-Active Agents; D020442:Poloxamer; D002734:Chlorophyll; C031183:stearic acid; C025343:monooctanoin
keywords: DH-I-180-3; Nanostructured lipid carriers; Photodynamic therapy; Solid lipid nanoparticle