Polymeric Nanocapsules Containing Kojic Acid Dipalmitate and Rosehip Oil - Development and Evaluation of Preliminary Efficacy and Safety for Skin Whitening

Sep 28, 2026

Uploaded by Miles

Polymeric nanocapsules combining kojic acid dipalmitate (KDP) with rosehip oil were developed to enable high-performance skin whitening/lightening while limiting KDP contact with external media and preventing degradation. Formulations containing 0.1% KDP and 5% rosehip oil were prepared using Eudragit RS100, Eudragit S100, PCL, and PLGA, producing particles under 200 nm with pH 2.5–5.0, 0.9 mg/mL KDP and >99% encapsulation. PLGA nanocapsules best preserved KDP over 180 days and delivered KDP to the epidermis, showed antioxidant activity in DPPH and β-carotene/linoleic acid assays, inhibited tyrosinase in vitro, reduced melanin in NHEM, and exhibited cytocompatibility in 3T3-L1 and NHEM.

LanguageEnglish

CategoryHealthcare

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Pages16

Reading Time40 min

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Abstract

Introduction

Kojic acid and limitations

Kojic acid dipalmitate as an alternative

Rosehip oil properties and stability

Nanotechnology and polymeric nanocapsules as delivery systems

This article is licensed under CC-BY 4.0 [http://pubs.acs.org/journal/acsodf](http://pubs.acs.org/journal/acsodf) Article Polymeric Nanocapsules Containing Kojic Acid Dipalmitate and Rosehip Oil: Development and Evaluation of Preliminary Efficacy and Safety for Skin Whitening J́ulia Capp Zilles, Marya Alexandrina Vallenot Lemos, Larissa Pedron Duarte, Maria Paula Faccin Huth, Irene Clemes Kulkamp Guerreiro, Bonnie C. Carney, Aline Rigon Zimmer, and Renata Vidor Contri* Cite This: ACS Omega 2025, 10, 62987−63002 Read Online | | | | | | --- | --- | --- | --- | | ACCESS | Metrics & More | | Article Recommendations | ABSTRACT: Polymeric nanocapsules associated with kojic acid dipalmitate (KDP) and rosehip oil can be a strategy to obtain highperformance skin whitening/lightning formulations. Nanocapsules containing 0.1% of KDP and 5% of rosehip oil were developed with different polymers (Eudragit RS100, Eudragit S100, poly(ε-caprolactone) (PCL) and poly(D,L-lactide-co-glycolide) (PLGA)) to limit the contact of KDP with the external media and avoid its degradation. The nanocapsules had a diameter of less than 200 nm, with suitable size distribution, a pH range between 2.5 and 5.0, a KDP content of 0.9 mg/mL and an encapsulation efficiency above 99%. The zeta potential was positive for the Eudragit RS100 nanocapsules and negative for the other nanocapsules. The PLGA nanocapsules were selected due to better stability results, since there was no decay in KDP content after 180 days (refrigerated storage). The in vitro skin permeation assay showed that KDP reaches the epidermis. This formulation showed in vitro antioxidant activity through both the DPPH assay and the β-carotene/linoleic acid assay when used at 25 μg/mL of KDP, with higher activity than a kojic acid solution (KDP correspondent concentration) and, at 13.75 μg/mL, inhibited tyrosinase in vitro to 17%, significantly greater than the kojic acid solution. A 25% melanin reduction was obtained after normal human epidermal melanocytes (NHEM) were treated with 3.1 μg/mL ofKDP. Cytocompatibility was observed after 24 h treatment with up to 6.25 μg/mL of the formulation in fibroblast-like cells (3T3-L1) and up to 3.1 μg/mL in NHEM. Therefore, PLGA nanocapsules containing KDP and rosehip oil have potential for use in skin whitening/lightning formulations. 1. INTRODUCTION The interest in developing cosmetic formulations containing effective and safe bioactive compounds has increased, especially in regards to their stability, skin penetration and skin compatibility.1 Kojic acid is an organic acid derived from fungi fermentation, such as Aspergillum and Penicillium, and it is widely studied for its skin whitening properties and its capacity to inhibit tyrosinase, the key enzyme in melanin synthesis.2 However, its use is limited because of its low stability, sensitivity to light and heat, and oxidation. Additionally, adverse effects such as contact dermatitis and skin irritation have been reported.3−5 To overcome the limitations of kojic acid, kojic acid derivatives, such as kojic acid dipalmitate (KDP), appear to be promising alternatives. KDP is the esterified form of kojic acid, and it is stable to light and heat and in a wide pH range without suffering color alterations.6,7 The KDP molecule is hydrolyzed by esterases located on the skin, releasing kojic acid | Received: August 29, 2025
Revised: December 1, 2025
Accepted: December 5, 2025
Published: December 12, 2025 | | | --- | --- | © 2025 The Authors. Published by American Chemical Society 62987 [https://doi.org/10.1021/acsomega.5c08878](https://doi.org/10.1021/acsomega.5c08878) ACS Omega 2025, 10, 62987−63002 Table 1. Components of Nanocapsules Suspensionsa NC ERS100 NC ES100 NC PCL NC PLGA/NC-R-KDP NC-R NC-T-KDP NC-T aKDP = kojic acid dipalmitate; PCL = poly(ε-caprolactone) (Mn 80,000); PLGA = poly(D,L-lactide-co-glycolide) 75/25; NC-R = PLGA nanocapsules with rosehip oil a

FAQs

What problem do polymeric nanocapsules solve for KDP formulations?

They limit KDP’s contact with the external environment to reduce degradation and improve formulation performance for skin whitening/lightening.

Which nanocapsule type showed the best stability for KDP?

PLGA nanocapsules showed better stability, with no decay in KDP content after 180 days of refrigerated storage.

What evidence supports skin-whitening potential in vitro?

In vitro permeation indicated KDP reaches the epidermis, antioxidant activity was observed (DPPH and β-carotene/linoleic acid assays), and tyrosinase inhibition and melanin reduction were reported in relevant cell-based testing.

Sep 28, 2026

Uploaded by Miles