Systematic study of drug distribution profiles of different nanocarriers in the skin layers: a more accurate and targeted delivery

The aim of this work was to evaluate the skin distributions of two drugs with different logarithm of the distribution coefficient (Log D) values. Melatonin (MEL; Log D 1.74) and benzophenone-3 (BZA-3; Log D 3.88) lipid core nanocapsules (LNCs) were prepared with poly(e-caprolactone) (PCL) of differ...

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Main Authors: Manuela Gonçalves, Kelly Cristine Zatta, Adriana Raffin Pohlmann, Silvia Stanisçuaski Guterres
Format: Article
Language:English
Published: Universidade Federal do Rio Grande do Sul 2024-12-01
Series:Drug Analytical Research
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Online Access:https://seer.ufrgs.br/rita/citati/index.php/dar/article/view/143983
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author Manuela Gonçalves
Kelly Cristine Zatta
Adriana Raffin Pohlmann
Silvia Stanisçuaski Guterres
author_facet Manuela Gonçalves
Kelly Cristine Zatta
Adriana Raffin Pohlmann
Silvia Stanisçuaski Guterres
author_sort Manuela Gonçalves
collection DOAJ
description The aim of this work was to evaluate the skin distributions of two drugs with different logarithm of the distribution coefficient (Log D) values. Melatonin (MEL; Log D 1.74) and benzophenone-3 (BZA-3; Log D 3.88) lipid core nanocapsules (LNCs) were prepared with poly(e-caprolactone) (PCL) of different molar weights (14,000 g mol-1 and 80,000 g mol-1), capric/caprylic triglyceride, sorbitan monostearate and polysorbate 80, and nanoemulsions (NE) were similarly prepared without polymer. In vitro release experiments combined with in vitro percutaneous penetration/permeation data demonstrated that the localization of the substance in the nanoparticles (determined by Log D) is crucial for understanding their diffusion behavior. The results demonstrated that substances of moderate lipophilicity, such as MEL, are affected by the molar mass of the polymer since the use of 80,000 g mol-1 PCL in the particle composition (LNC80MEL) guaranteed a greater encapsulation efficiency (EE%) (55%). On the other hand, the percutaneous distribution profile of substances with high lipophilicity, such as BZA-3, is not influenced by the molar mass of the polymer since for all formulations containing BZA-3, the EE% was approximately 99%. However, the presence of a polymer in the nanocapsule (LNC) tends to promote greater retention of the substance at the stratum corneum level, while its absence (NE) allows penetration of the particle through the skin layers and drives a higher concentration of BZA-3 into the dermis.  
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spelling doaj-art-195005071dc841d7961261c992f8d4872025-01-07T18:21:24ZengUniversidade Federal do Rio Grande do SulDrug Analytical Research2527-26162024-12-018210.22456/2527-2616.143983Systematic study of drug distribution profiles of different nanocarriers in the skin layers: a more accurate and targeted deliveryManuela Gonçalves0Kelly Cristine ZattaAdriana Raffin PohlmannSilvia Stanisçuaski GuterresUFRGS The aim of this work was to evaluate the skin distributions of two drugs with different logarithm of the distribution coefficient (Log D) values. Melatonin (MEL; Log D 1.74) and benzophenone-3 (BZA-3; Log D 3.88) lipid core nanocapsules (LNCs) were prepared with poly(e-caprolactone) (PCL) of different molar weights (14,000 g mol-1 and 80,000 g mol-1), capric/caprylic triglyceride, sorbitan monostearate and polysorbate 80, and nanoemulsions (NE) were similarly prepared without polymer. In vitro release experiments combined with in vitro percutaneous penetration/permeation data demonstrated that the localization of the substance in the nanoparticles (determined by Log D) is crucial for understanding their diffusion behavior. The results demonstrated that substances of moderate lipophilicity, such as MEL, are affected by the molar mass of the polymer since the use of 80,000 g mol-1 PCL in the particle composition (LNC80MEL) guaranteed a greater encapsulation efficiency (EE%) (55%). On the other hand, the percutaneous distribution profile of substances with high lipophilicity, such as BZA-3, is not influenced by the molar mass of the polymer since for all formulations containing BZA-3, the EE% was approximately 99%. However, the presence of a polymer in the nanocapsule (LNC) tends to promote greater retention of the substance at the stratum corneum level, while its absence (NE) allows penetration of the particle through the skin layers and drives a higher concentration of BZA-3 into the dermis.   https://seer.ufrgs.br/rita/citati/index.php/dar/article/view/143983Lipid core nanocapsulenanoemulsionLog Dskin penetrationskin permeationin vitro release
spellingShingle Manuela Gonçalves
Kelly Cristine Zatta
Adriana Raffin Pohlmann
Silvia Stanisçuaski Guterres
Systematic study of drug distribution profiles of different nanocarriers in the skin layers: a more accurate and targeted delivery
Drug Analytical Research
Lipid core nanocapsule
nanoemulsion
Log D
skin penetration
skin permeation
in vitro release
title Systematic study of drug distribution profiles of different nanocarriers in the skin layers: a more accurate and targeted delivery
title_full Systematic study of drug distribution profiles of different nanocarriers in the skin layers: a more accurate and targeted delivery
title_fullStr Systematic study of drug distribution profiles of different nanocarriers in the skin layers: a more accurate and targeted delivery
title_full_unstemmed Systematic study of drug distribution profiles of different nanocarriers in the skin layers: a more accurate and targeted delivery
title_short Systematic study of drug distribution profiles of different nanocarriers in the skin layers: a more accurate and targeted delivery
title_sort systematic study of drug distribution profiles of different nanocarriers in the skin layers a more accurate and targeted delivery
topic Lipid core nanocapsule
nanoemulsion
Log D
skin penetration
skin permeation
in vitro release
url https://seer.ufrgs.br/rita/citati/index.php/dar/article/view/143983
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AT kellycristinezatta systematicstudyofdrugdistributionprofilesofdifferentnanocarriersintheskinlayersamoreaccurateandtargeteddelivery
AT adrianaraffinpohlmann systematicstudyofdrugdistributionprofilesofdifferentnanocarriersintheskinlayersamoreaccurateandtargeteddelivery
AT silviastaniscuaskiguterres systematicstudyofdrugdistributionprofilesofdifferentnanocarriersintheskinlayersamoreaccurateandtargeteddelivery