Abstract
Background: Hyperpigmentation is a common disorder characterized by brown patches, differential skin tone, and sunburns on the area of exposure. Hydroquinone (HQ) is considered the most effective agent in the treatment of pigmentation but exhibits skin irritation and local toxicity at higher concentrations. Hence, HQ-encapsulated nanostructured lipid carriers (NLCs) were designed and assessed as an alternative for the treatment of pigmentation to reduce skin irritation without exhibiting toxicity.
Objective: The objective of this study was to formulate and evaluate hydroquinone-encapsulated NLCs in the cream base as a treatment for hyperpigmentation.
Methods: The present formulation aimed to encapsulate adequate hydroquinone in NLCs for potential application of depigmentation. Hydroquinone was formulated utilizing meltemulsification ultrasound dispersion technique, in which the aqueous phase consists of water and Tween 80, whereas the lipid phase is prepared with oleic acid and glyceryl monostearate. The characteristics of the final formulation were analyzed by surface morphology, percentage entrapment efficiency, ex-vivo release, in-vitro release, and cell line studies.
Results: Hydroquinone-encapsulated lipid nanocarriers demonstrated promising results within the size range of 22 ± 1.22 nm to 164 ± 0.75 nm and encapsulation efficiency of 78 ± 5.05 % in a partially crystallized lipid-based state. The system displayed enhancement in absorption and penetration with zeta potential of -10.2 ± 1.86 mV to -24.6 ± 0.45 mV, and presented a substantial decrease in water loss as a result of packet formation.
Conclusion: The results indicated hydroquinone-encapsulated NLCs as safe and effective for the treatment of pigmented skin, reducing the appearance of dark patches and improving the skin texture.
Keywords: NLC, skin whitening, hydroquinone, emulsification ultrasound dispersion, hyperpigmentation, delivery systems
Graphical Abstract
[http://dx.doi.org/10.3390/cosmetics3030027]
[http://dx.doi.org/10.1111/jdv.13595]
[http://dx.doi.org/10.1016/j.ijpharm.2017.04.020] [PMID: 28416402]
[http://dx.doi.org/10.1001/jama.1965.03090220021006] [PMID: 5897965]
[http://dx.doi.org/10.1002/ptr.1954] [PMID: 16841367]
[http://dx.doi.org/10.1111/j.1468-3083.2006.01670.x] [PMID: 16898897]
[http://dx.doi.org/10.3109/09687688.2010.510804] [PMID: 20939772]
[http://dx.doi.org/10.1016/S0190-9622(81)70082-3] [PMID: 7021611]
[http://dx.doi.org/10.1111/1523-1747.ep12701679] [PMID: 4206837]
[http://dx.doi.org/10.1111/j.1365-2133.1995.tb02660.x] [PMID: 8546987]
[http://dx.doi.org/10.1111/1523-1747.ep12260588] [PMID: 6200545]
[http://dx.doi.org/10.1016/j.xphs.2017.02.026] [PMID: 28259767]
[http://dx.doi.org/10.1016/S0168-3659(97)01653-2]
[http://dx.doi.org/10.1016/j.colsurfb.2015.10.041] [PMID: 26579567]
[http://dx.doi.org/10.15171/apb.2016.072] [PMID: 28101465]
[http://dx.doi.org/10.3390/scipharm84040634]
[http://dx.doi.org/10.1155/2017/3282693]
[http://dx.doi.org/10.1016/j.biopha.2018.04.055] [PMID: 29677547]
[http://dx.doi.org/10.1016/j.bfopcu.2015.10.001]
[http://dx.doi.org/10.1016/j.ejpb.2013.08.013] [PMID: 24007657]
[http://dx.doi.org/10.3390/nano7060122] [PMID: 28554993]
[http://dx.doi.org/10.1016/j.ejpb.2009.12.008] [PMID: 20060469]
[http://dx.doi.org/10.1016/j.ijpharm.2008.01.045] [PMID: 18343059]
[http://dx.doi.org/10.1016/j.bbrc.2008.03.127] [PMID: 18395002]
[http://dx.doi.org/10.1016/j.ijpharm.2010.03.032] [PMID: 20302925]
[http://dx.doi.org/10.1186/s12935-018-0596-x] [PMID: 30008618]
[http://dx.doi.org/10.3109/10837450.2014.996900] [PMID: 25560648]