Nanostructured lipid carrier-loaded hyaluronic acid microneedles for controlled dermal delivery of a lipophilic molecule

Sang Gon Lee, Jae Han Jeong, Kyung Min Lee, Kyu Ho Jeong, Huisuk Yang, Miroo Kim, Hyungil Jung, Sangkil Lee, Young Wook Choi

Research output: Contribution to journalArticle

35 Citations (Scopus)

Abstract

Nanostructured lipid carriers (NLCs) were employed to formulate a lipophilic drug into hydrophilic polymeric microneedles (MNs). Hyaluronic acid (HA) was selected as a hydrophilic and bioerodible polymer to fabricate MNs, and nile red (NR) was used as a model lipophilic molecule. NR-loaded NLCs were consolidated into the HA-based MNs to prepare NLC-loaded MNs (NLC-MNs). A dispersion of NLCs was prepared by high-pressure homogenization after dissolving NR in Labrafil and mixing with melted Compritol, resulting in 268 nm NLCs with a polydispersity index of 0.273. The NLC dispersion showed a controlled release of NR over 24hours, following Hixson-Crowell's cube root law. After mixing the NLC dispersion with the HA solution, the drawing lithography method was used to fabricate NLC MNs. The length, base diameter, and tip diameter of the NLC-MNs were approximately 350, 380, and 30μm, respectively. Fluorescence microscopic imaging of the NLC-MNs helped confirm that the NR-loaded NLCs were distributed evenly throughout the MNs. In a skin permeation study performed using a Franz diffusion cell with minipig dorsal skin, approximately 70% of NR was localized in the skin after 24-hour application of NLC-MNs. Confocal laser scanning microscopy (z-series) of the skin at different depths showed strong fluorescence intensity in the epidermal layer, which appeared to spread out radially with the passage of time. This study indicated that incorporation of drug-loaded NLCs into MNs could represent a promising strategy for controlled dermal delivery of lipophilic drugs.

Original languageEnglish
Pages (from-to)289-299
Number of pages11
JournalInternational journal of nanomedicine
Volume9
Issue number1
DOIs
Publication statusPublished - 2013 Dec 31

Fingerprint

Hyaluronic acid
Hyaluronic Acid
Lipids
Skin
Molecules
Fluorescence
Pharmaceutical Preparations
Miniature Swine
Optical Imaging
Polydispersity
Confocal Microscopy
Permeation
Lithography
nile red

All Science Journal Classification (ASJC) codes

  • Biophysics
  • Bioengineering
  • Biomaterials
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

Cite this

Lee, Sang Gon ; Jeong, Jae Han ; Lee, Kyung Min ; Jeong, Kyu Ho ; Yang, Huisuk ; Kim, Miroo ; Jung, Hyungil ; Lee, Sangkil ; Choi, Young Wook. / Nanostructured lipid carrier-loaded hyaluronic acid microneedles for controlled dermal delivery of a lipophilic molecule. In: International journal of nanomedicine. 2013 ; Vol. 9, No. 1. pp. 289-299.
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abstract = "Nanostructured lipid carriers (NLCs) were employed to formulate a lipophilic drug into hydrophilic polymeric microneedles (MNs). Hyaluronic acid (HA) was selected as a hydrophilic and bioerodible polymer to fabricate MNs, and nile red (NR) was used as a model lipophilic molecule. NR-loaded NLCs were consolidated into the HA-based MNs to prepare NLC-loaded MNs (NLC-MNs). A dispersion of NLCs was prepared by high-pressure homogenization after dissolving NR in Labrafil and mixing with melted Compritol, resulting in 268 nm NLCs with a polydispersity index of 0.273. The NLC dispersion showed a controlled release of NR over 24hours, following Hixson-Crowell's cube root law. After mixing the NLC dispersion with the HA solution, the drawing lithography method was used to fabricate NLC MNs. The length, base diameter, and tip diameter of the NLC-MNs were approximately 350, 380, and 30μm, respectively. Fluorescence microscopic imaging of the NLC-MNs helped confirm that the NR-loaded NLCs were distributed evenly throughout the MNs. In a skin permeation study performed using a Franz diffusion cell with minipig dorsal skin, approximately 70{\%} of NR was localized in the skin after 24-hour application of NLC-MNs. Confocal laser scanning microscopy (z-series) of the skin at different depths showed strong fluorescence intensity in the epidermal layer, which appeared to spread out radially with the passage of time. This study indicated that incorporation of drug-loaded NLCs into MNs could represent a promising strategy for controlled dermal delivery of lipophilic drugs.",
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Nanostructured lipid carrier-loaded hyaluronic acid microneedles for controlled dermal delivery of a lipophilic molecule. / Lee, Sang Gon; Jeong, Jae Han; Lee, Kyung Min; Jeong, Kyu Ho; Yang, Huisuk; Kim, Miroo; Jung, Hyungil; Lee, Sangkil; Choi, Young Wook.

In: International journal of nanomedicine, Vol. 9, No. 1, 31.12.2013, p. 289-299.

Research output: Contribution to journalArticle

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AU - Jeong, Jae Han

AU - Lee, Kyung Min

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AU - Yang, Huisuk

AU - Kim, Miroo

AU - Jung, Hyungil

AU - Lee, Sangkil

AU - Choi, Young Wook

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