Development of Propolis (Apis trigona)-loaded Nanoemulgel for Improved Skin Penetration of Caffeic Acid: The Effect of Variation of Oleic Acid Concentration

Afdil Viqar Viqhi; Marianti A. Manggau; Sartini Sartini; Elly Wahyudin; Latifah Rahman; Risfah Yulianti; Andi Dian Permana; Satria Aztasaury Awal

doi:10.3889/oamjms.2021.6672

Authors

Afdil Viqar Viqhi Postgraduate, Faculty of Pharmacy, Hasanuddin University, Makassar, South Sulawesi, Indonesia https://orcid.org/0000-0001-9962-8698
Marianti A. Manggau Department of Pharmacology and Toxicology, Faculty of Pharmacy, Hasanuddin University, Makassar, South Sulawesi, Indonesia
Sartini Sartini Department of Pharmaceutics, Faculty of Pharmacy, Hasanuddin University, Makassar, South Sulawesi, Indonesia
Elly Wahyudin Department of Pharmacology and Toxicology, Faculty of Pharmacy, Hasanuddin University, Makassar, South Sulawesi, Indonesia
Latifah Rahman Department of Pharmaceutics, Faculty of Pharmacy, Hasanuddin University, Makassar, South Sulawesi, Indonesia
Risfah Yulianti Department of Chemical Pharmacy, Faculty of Pharmacy, Hasanuddin University, Makassar, South Sulawesi, Indonesia
Andi Dian Permana Department of Pharmaceutics, Faculty of Pharmacy, Hasanuddin University, Makassar, South Sulawesi, Indonesia
Satria Aztasaury Awal Postgraduate, Faculty of Pharmacy, Hasanuddin University, Makassar, South Sulawesi, Indonesia

DOI:

https://doi.org/10.3889/oamjms.2021.6672

Keywords:

Propolis, Nanoemulgel, Caffeic acid, Oleic acid, Penetration

Abstract

BACKGROUND: Propolis contains caffeic acid compounds, which are proven to have pharmacological effects as an anti-inflammatory. However, its effectiveness is hampered by the poor solubility of caffeic acid. Here, we report developing the nanoemulgel approach containing propolis extract as an active ingredient and oleic acid as a permeation enhancer for transdermal delivery of caffeic acid.

AIM: This study aims to determine the effect of oleic acid concentration on increasing caffeic acid permeation in the skin and obtain a nanoemulgel formula with desired physical characteristics and stability.

MATERIALS AND METHODS: Propolis was macerated with 70% ethanol; the total phenolic content was measured by ultraviolet–visible spectrophotometer, and the levels of caffeic acid in the extracts and nanoemulgel preparations were finally determined using ultra-fast liquid chromatography. Formulas were made using various concentrations of oleic acid, namely, 1.25%w/w (Formula F1); 2.5%w/w (Formula F2); 5%w/w (Formula F3), respectively; and 1.25%w/w without propolis extract (Formula F4) as a comparison.

RESULTS: The results obtained from analysis of variance statistical exhibited that the difference in oleic acid concentrations in four formulas significantly affected (p < 0.05) particle size, polydispersity index, spreadability, adhesion, freeze-thaw, permeation, and retention test. However, there was no significant difference (p > 0.05) on pH and viscosity before and after 4 weeks of storage and zeta potential test. The highest amount of permeation and retention was found in F3 and F2, respectively, and all formulas tended to follow zero-order drug release kinetics. Furthermore, the results showed that the number of percent’s permeated in a row was 3.74% (F1); 5.58% (F2); 11.67% (F3), and F2 was the formula with the most optimal retention amount with a percentage of 43.13% at 24 h.

CONCLUSION: This study shows a promising delivery system for increasing the effectiveness of natural lipophilic compounds to treat inflammation in the skin.

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