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Topical delivery of Idebenone using nanostructured lipid carriers: evaluations of sun-protection and anti-oxidant effects

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Abstract

The objective of present study was to develop nanostructured lipid carriers (NLC) for topical delivery of antioxidant drug and evaluation of its sun protection efficacy. In the present study attempts have been made to formulate Idebenone loaded nanostructured lipid carriers (INLC) by using solvent precipitation method. Preformulation study evidenced for selection of Captex 500 P as an oil phase in which Idebenone has saturation solubility of 0.266 ± 0.032 g/ml. Compritol 888 ATO and ethanol were selected as solid lipid and solvent respectively. Surfactant and co-surfactant as Labrasol and Transcutol P have given stable formulations on the basis of HLB required for stabilization, respect to oil phase. INLC has particle size of 605 ± 4.01 nm and %EE of 82.58 ± 2.20 %. Optimized batches were subjected for crystallographic investigation, in vitro skin permeation study, drug deposition study, SPF determination and antioxidant activity. XRD, DSC studies illustrated that partial amorphization of Idebenone by molecularly dispersion within lipid blend leads for entrapment of drug. Permeation data showed that optimized INLC has flux value (Jss) of 7.87 μg cm−2 h−1. High significance (P < 0.001) of drug deposition in skin was observed between INLC and plain Idebenone gel. SPF value for INLC has 23 which represents that lipid nanocarriers have standards of blocking of 94–96 % of UVB rays. Such high skin deposition and SPF leads to more antioxidant effect of formulations. Hence lipid nanocarriers such as NLC have potential as an antioxidant and sun protection for topical drug delivery.

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Abbreviations

SLN:

Solid lipid nanoparticles

NLC:

Nanostructured lipid carriers

INLC:

Idebenone loaded nanostructured lipid carriers

NE:

Nanoemulsions

HLB:

Hydrophilic lipophilic balance

XRD:

X-ray crystallography

DSC:

Differential scanning calorimetry

TEM:

Transmission electron microscopy

DDW:

Double distilled water

CPCSEA:

Committee for purpose, control and supervision of experimentation on animals

IAEC:

Institutional animal ethical committee

PBS:

Phosphate buffer saline

SPF:

Sun protection factor

DPPH 1:

1-Diphenyl-2-picrylhydrazyl

LD:

Laser diffractometer

MED:

Minimal erythema dose

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Acknowledgments

The authors are very thankful to Principal, Poona College of Pharmacy, Pune and Principal, Bharati Vidyapeeth College of Pharmacy, Kolhapur for providing necessary facilities for this research work. The authors are highly thankful to Biocon., Bangalore, India for providing Idebenone as a gift sample.

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Authors and Affiliations

  1. Department of Quality Assurance, Bharati Vidyapeeth College of Pharmacy, Near Chitranagari, Kolhapur, 416 013, Maharashtra, India

    Sachin S. Salunkhe & Neela M. Bhatia

  2. Department of Pharmaceutics, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Erandwane, Pune, 411 038, Maharashtra, India

    Varsha B. Pokharkar

  3. Department of Pharmaceutics, Bharati Vidyapeeth College of Pharmacy, Near Chitranagari, Kolhapur, 416 013, Maharashtra, India

    Jyoti D. Thorat

  4. Department of Pharmaceutical Chemistry, Bharati Vidyapeeth College of Pharmacy, Near Chitranagari, Kolhapur, 416 013, Maharashtra, India

    Manish S. Bhatia

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  1. Sachin S. Salunkhe
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  2. Neela M. Bhatia
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  3. Varsha B. Pokharkar
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Correspondence to Sachin S. Salunkhe.

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Salunkhe, S.S., Bhatia, N.M., Pokharkar, V.B. et al. Topical delivery of Idebenone using nanostructured lipid carriers: evaluations of sun-protection and anti-oxidant effects. Journal of Pharmaceutical Investigation 43, 287–303 (2013). https://doi.org/10.1007/s40005-013-0079-y

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