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Transdermal Delivery of Small Interfering RNA with Elastic Cationic Liposomes in Mice.

Hattori Y, Date M, Arai S, Kawano K, Yonemochi E, Maitani Y - J Pharm (Cairo) (2013)

Bottom Line: Although the sizes of all elastic liposomes prepared in this study were about 80-90 nm, the sizes of C5-, C10- and C15-liposome/siRNA complexes (lipoplexes) were about 1,700-1,800 nm, and those of T5-, T10-, and T15-lipoplexes were about 550-780 nm.Following skin application of the fluorescence-labeled lipoplexes in mice, among the elastic lipoplexes, C15- and T5-lipoplexes showed effective penetration of siRNA into skin, compared with DOTAP lipoplex and free siRNA solution.These data suggest that elastic cationic liposomes containing an appropriate amount of NaChol or Tween 80 as an edge activator could deliver siRNA transdermally.

View Article: PubMed Central - PubMed

Affiliation: Institute of Medicinal Chemistry, Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo 142-8501, Japan.

ABSTRACT
We developed elastic cationic liposomal vectors for transdermal siRNA delivery. These liposomes were prepared with 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) as a cationic lipid and sodium cholate (NaChol) or Tween 80 as an edge activator. When NaChol or Tween 80 was included at 5, 10, and 15% (w/w) into DOTAP liposomal formulations (C5-, C10-, and C15-liposomes and T5-, T10-, and T15-liposomes), C15- and T10-liposomes showed 2.4- and 2.7-fold-higher elasticities than DOTAP liposome, respectively. Although the sizes of all elastic liposomes prepared in this study were about 80-90 nm, the sizes of C5-, C10- and C15-liposome/siRNA complexes (lipoplexes) were about 1,700-1,800 nm, and those of T5-, T10-, and T15-lipoplexes were about 550-780 nm. Their elastic lipoplexes showed strong gene suppression by siRNA without cytotoxicity when transfected into human cervical carcinoma SiHa cells. Following skin application of the fluorescence-labeled lipoplexes in mice, among the elastic lipoplexes, C15- and T5-lipoplexes showed effective penetration of siRNA into skin, compared with DOTAP lipoplex and free siRNA solution. These data suggest that elastic cationic liposomes containing an appropriate amount of NaChol or Tween 80 as an edge activator could deliver siRNA transdermally.

No MeSH data available.


Related in: MedlinePlus

Effect of Tween 80 or NaChol content (w/w) on elasticity values of cationic elastic liposomes. Elasticity values were calculated by Jflux × (rv/rp)2. Each value represents the mean ± S.D. (n = 3).
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fig1: Effect of Tween 80 or NaChol content (w/w) on elasticity values of cationic elastic liposomes. Elasticity values were calculated by Jflux × (rv/rp)2. Each value represents the mean ± S.D. (n = 3).

Mentions: Next, we confirmed the deformability of the elastic liposomes. As shown in Figure 1, the elasticity of liposomes containing Tween 80 peaked at 10% (w/w) Tween 80 content and was reduced at 15% (w/w). T10-liposomes showed 2.7-fold-higher elasticity than DOTAP liposomes. In contrast, the elasticity of liposomes containing NaChol was increased with an increase of NaChol content, and C15-liposome showed 2.4-fold-higher elasticity than DOTAP liposome. These findings indicate that the optimal amount of edge activator for elasticity of DOTAP liposome differed between the liposomes containing NaChol and Tween 80.


Transdermal Delivery of Small Interfering RNA with Elastic Cationic Liposomes in Mice.

Hattori Y, Date M, Arai S, Kawano K, Yonemochi E, Maitani Y - J Pharm (Cairo) (2013)

Effect of Tween 80 or NaChol content (w/w) on elasticity values of cationic elastic liposomes. Elasticity values were calculated by Jflux × (rv/rp)2. Each value represents the mean ± S.D. (n = 3).
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4590792&req=5

fig1: Effect of Tween 80 or NaChol content (w/w) on elasticity values of cationic elastic liposomes. Elasticity values were calculated by Jflux × (rv/rp)2. Each value represents the mean ± S.D. (n = 3).
Mentions: Next, we confirmed the deformability of the elastic liposomes. As shown in Figure 1, the elasticity of liposomes containing Tween 80 peaked at 10% (w/w) Tween 80 content and was reduced at 15% (w/w). T10-liposomes showed 2.7-fold-higher elasticity than DOTAP liposomes. In contrast, the elasticity of liposomes containing NaChol was increased with an increase of NaChol content, and C15-liposome showed 2.4-fold-higher elasticity than DOTAP liposome. These findings indicate that the optimal amount of edge activator for elasticity of DOTAP liposome differed between the liposomes containing NaChol and Tween 80.

Bottom Line: Although the sizes of all elastic liposomes prepared in this study were about 80-90 nm, the sizes of C5-, C10- and C15-liposome/siRNA complexes (lipoplexes) were about 1,700-1,800 nm, and those of T5-, T10-, and T15-lipoplexes were about 550-780 nm.Following skin application of the fluorescence-labeled lipoplexes in mice, among the elastic lipoplexes, C15- and T5-lipoplexes showed effective penetration of siRNA into skin, compared with DOTAP lipoplex and free siRNA solution.These data suggest that elastic cationic liposomes containing an appropriate amount of NaChol or Tween 80 as an edge activator could deliver siRNA transdermally.

View Article: PubMed Central - PubMed

Affiliation: Institute of Medicinal Chemistry, Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo 142-8501, Japan.

ABSTRACT
We developed elastic cationic liposomal vectors for transdermal siRNA delivery. These liposomes were prepared with 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) as a cationic lipid and sodium cholate (NaChol) or Tween 80 as an edge activator. When NaChol or Tween 80 was included at 5, 10, and 15% (w/w) into DOTAP liposomal formulations (C5-, C10-, and C15-liposomes and T5-, T10-, and T15-liposomes), C15- and T10-liposomes showed 2.4- and 2.7-fold-higher elasticities than DOTAP liposome, respectively. Although the sizes of all elastic liposomes prepared in this study were about 80-90 nm, the sizes of C5-, C10- and C15-liposome/siRNA complexes (lipoplexes) were about 1,700-1,800 nm, and those of T5-, T10-, and T15-lipoplexes were about 550-780 nm. Their elastic lipoplexes showed strong gene suppression by siRNA without cytotoxicity when transfected into human cervical carcinoma SiHa cells. Following skin application of the fluorescence-labeled lipoplexes in mice, among the elastic lipoplexes, C15- and T5-lipoplexes showed effective penetration of siRNA into skin, compared with DOTAP lipoplex and free siRNA solution. These data suggest that elastic cationic liposomes containing an appropriate amount of NaChol or Tween 80 as an edge activator could deliver siRNA transdermally.

No MeSH data available.


Related in: MedlinePlus