A formulation study of 5-aminolevulinic encapsulated in DPPC liposomes in melanoma treatment

Ming Wei Lin, Yaw Bin Huang, Chun Lin Chen, Pao Chu Wu, Chien Ying Chou, Ping Ching Wu, Shih Ya Hung

研究成果: Article

11 引文 (Scopus)

摘要

Photodynamic therapy (PDT) is a widely used technique for epithelial skin cancer treatment. 5-aminolevulinic acid (5-ALA) is a drug currently used for PDT and is a hydrophilic molecule at its physiological pH, and this limits its capacity to cross the stratum corneum of skin. Since skin penetration is a key factor in the efficacy of topical 5-ALA-mediated PDT, numerous strategies have been proposed to improve skin penetration. Yet this problem is still ongoing. The results of a previous study showed a low rate of 5-ALA encapsulated in liposomes (5.7%) that were 400 nm in size. In the present study, we used 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) liposomes as vehicles and tested their delivery efficacy of 5-ALA-medicated PDT both in vitro and in vivo. Our data shows that 5-ALA encapsulated in 0.1 or 0.5% DPPC liposomes (5-ALA/DPPC) had a better encapsulated rate (15~16%) and were smaller in size (84~89 nm). We found the 5-ALA/DPPC formulation reduced cell viability, mitochondria membrane potential, and enhanced intracellular ROS accumulation as compared to 5-ALA alone in melanoma cells. Furthermore, the 5-ALA/DPPC formulation also had better skin penetration ability as compared to the 5-ALA in our ex vivo data by assaying 5-ALA converted into protoporphyrin IX (PpIX) in the skin of the mice that were experimented on. In melanoma xenograft models, 5-ALA/DPPC enhanced PpIX accumulation only in tumor tissue but not normal skin. In conclusion, we found DPPC liposomes to be good carriers for 5-ALA delivery and believe that they may prove useful in 5-ALA-mediated PDT in the future.

原文English
頁(從 - 到)483-489
頁數7
期刊International Journal of Medical Sciences
13
發行號7
DOIs
出版狀態Published - 2016 六月 18

指紋

Aminolevulinic Acid
Phosphorylcholine
Liposomes
Melanoma
Photochemotherapy
Skin
Therapeutics
Skin Neoplasms
Heterografts
Membrane Potentials
Cornea
Cell Survival
Mitochondria

All Science Journal Classification (ASJC) codes

  • Medicine(all)

引用此文

Lin, Ming Wei ; Huang, Yaw Bin ; Chen, Chun Lin ; Wu, Pao Chu ; Chou, Chien Ying ; Wu, Ping Ching ; Hung, Shih Ya. / A formulation study of 5-aminolevulinic encapsulated in DPPC liposomes in melanoma treatment. 於: International Journal of Medical Sciences. 2016 ; 卷 13, 編號 7. 頁 483-489.
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title = "A formulation study of 5-aminolevulinic encapsulated in DPPC liposomes in melanoma treatment",
abstract = "Photodynamic therapy (PDT) is a widely used technique for epithelial skin cancer treatment. 5-aminolevulinic acid (5-ALA) is a drug currently used for PDT and is a hydrophilic molecule at its physiological pH, and this limits its capacity to cross the stratum corneum of skin. Since skin penetration is a key factor in the efficacy of topical 5-ALA-mediated PDT, numerous strategies have been proposed to improve skin penetration. Yet this problem is still ongoing. The results of a previous study showed a low rate of 5-ALA encapsulated in liposomes (5.7{\%}) that were 400 nm in size. In the present study, we used 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) liposomes as vehicles and tested their delivery efficacy of 5-ALA-medicated PDT both in vitro and in vivo. Our data shows that 5-ALA encapsulated in 0.1 or 0.5{\%} DPPC liposomes (5-ALA/DPPC) had a better encapsulated rate (15~16{\%}) and were smaller in size (84~89 nm). We found the 5-ALA/DPPC formulation reduced cell viability, mitochondria membrane potential, and enhanced intracellular ROS accumulation as compared to 5-ALA alone in melanoma cells. Furthermore, the 5-ALA/DPPC formulation also had better skin penetration ability as compared to the 5-ALA in our ex vivo data by assaying 5-ALA converted into protoporphyrin IX (PpIX) in the skin of the mice that were experimented on. In melanoma xenograft models, 5-ALA/DPPC enhanced PpIX accumulation only in tumor tissue but not normal skin. In conclusion, we found DPPC liposomes to be good carriers for 5-ALA delivery and believe that they may prove useful in 5-ALA-mediated PDT in the future.",
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A formulation study of 5-aminolevulinic encapsulated in DPPC liposomes in melanoma treatment. / Lin, Ming Wei; Huang, Yaw Bin; Chen, Chun Lin; Wu, Pao Chu; Chou, Chien Ying; Wu, Ping Ching; Hung, Shih Ya.

於: International Journal of Medical Sciences, 卷 13, 編號 7, 18.06.2016, p. 483-489.

研究成果: Article

TY - JOUR

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AU - Lin, Ming Wei

AU - Huang, Yaw Bin

AU - Chen, Chun Lin

AU - Wu, Pao Chu

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AU - Wu, Ping Ching

AU - Hung, Shih Ya

PY - 2016/6/18

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AB - Photodynamic therapy (PDT) is a widely used technique for epithelial skin cancer treatment. 5-aminolevulinic acid (5-ALA) is a drug currently used for PDT and is a hydrophilic molecule at its physiological pH, and this limits its capacity to cross the stratum corneum of skin. Since skin penetration is a key factor in the efficacy of topical 5-ALA-mediated PDT, numerous strategies have been proposed to improve skin penetration. Yet this problem is still ongoing. The results of a previous study showed a low rate of 5-ALA encapsulated in liposomes (5.7%) that were 400 nm in size. In the present study, we used 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) liposomes as vehicles and tested their delivery efficacy of 5-ALA-medicated PDT both in vitro and in vivo. Our data shows that 5-ALA encapsulated in 0.1 or 0.5% DPPC liposomes (5-ALA/DPPC) had a better encapsulated rate (15~16%) and were smaller in size (84~89 nm). We found the 5-ALA/DPPC formulation reduced cell viability, mitochondria membrane potential, and enhanced intracellular ROS accumulation as compared to 5-ALA alone in melanoma cells. Furthermore, the 5-ALA/DPPC formulation also had better skin penetration ability as compared to the 5-ALA in our ex vivo data by assaying 5-ALA converted into protoporphyrin IX (PpIX) in the skin of the mice that were experimented on. In melanoma xenograft models, 5-ALA/DPPC enhanced PpIX accumulation only in tumor tissue but not normal skin. In conclusion, we found DPPC liposomes to be good carriers for 5-ALA delivery and believe that they may prove useful in 5-ALA-mediated PDT in the future.

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