TY - JOUR
T1 - Hydrogel composite containing azelaic acid and tea tree essential oil as a therapeutic strategy for Propionibacterium and testosterone-induced acne
AU - Bisht, Alpna
AU - Hemrajani, Chetna
AU - Rathore, Charul
AU - Dhiman, Tania
AU - Rolta, Rajan
AU - Upadhyay, Navneet
AU - Nidhi, Prakriti
AU - Gupta, Gaurav
AU - Dua, Kamal
AU - Chellappan, Dinesh Kumar
AU - Dev, Kamal
AU - Sourirajan, Anuradha
AU - Chakraborty, Apala
AU - Aljabali, Alaa A A
AU - Bakshi, Hamid A
AU - Negi, Poonam
AU - Tambuwala, Murtaza M
N1 - © 2021. The Author(s).
PY - 2022/10
Y1 - 2022/10
N2 - Azelaic acid (AzA) is a USFDA bioactive prescribed against acne vulgaris. It possesses delivery challenges like poor aqueous solubility, low skin-penetrability, and dose-dependent side effects, which could be overcome by its synergistic combination with tea tree oil (TTO) as a microemulsion (ME)-based hydrogel composite. AzA-TTO ME was prepared to employ pseudo-ternary phase diagram construction. The best AzA-TTO ME was of uniform size (polydispersity index < 0.7), nano-range (~357.4 ± 2% nm), transmittance (> 90%), and negative zeta potential (-1.42 ± 0.25% mV) values. ME hydrogel composite with optimum rheological and textural attributes showed better permeation, retention, and skin-compliant characteristics, vis-a-vis marketed formulation (Aziderm™) when evaluated in Wistar rat skin. In vitro antibacterial efficacy in bacterial strains, i.e., Staphylococcus aureus, Propionibacterium acne, and Staphylococcus epidermidis, was evaluated employing agar well plate diffusion and broth dilution assay. ME hydrogel has shown an increase in zone of inhibition by two folds and a decrease in minimum inhibitory concentration (MIC) by eightfold against P. acnes vis-a-vis AzA. Finally, ME hydrogel composite exhibited a better reduction in the papule density (93.75 ± 1.64%) in comparison to Aziderm™ 72.69 ± 4.67%) on acne as developed in rats by inducing testosterone. Thus, the developed AzA-TTO ME hydrogel composite promises an efficacious and comparatively safer drug delivery system for the topical therapy of acne vulgaris.
AB - Azelaic acid (AzA) is a USFDA bioactive prescribed against acne vulgaris. It possesses delivery challenges like poor aqueous solubility, low skin-penetrability, and dose-dependent side effects, which could be overcome by its synergistic combination with tea tree oil (TTO) as a microemulsion (ME)-based hydrogel composite. AzA-TTO ME was prepared to employ pseudo-ternary phase diagram construction. The best AzA-TTO ME was of uniform size (polydispersity index < 0.7), nano-range (~357.4 ± 2% nm), transmittance (> 90%), and negative zeta potential (-1.42 ± 0.25% mV) values. ME hydrogel composite with optimum rheological and textural attributes showed better permeation, retention, and skin-compliant characteristics, vis-a-vis marketed formulation (Aziderm™) when evaluated in Wistar rat skin. In vitro antibacterial efficacy in bacterial strains, i.e., Staphylococcus aureus, Propionibacterium acne, and Staphylococcus epidermidis, was evaluated employing agar well plate diffusion and broth dilution assay. ME hydrogel has shown an increase in zone of inhibition by two folds and a decrease in minimum inhibitory concentration (MIC) by eightfold against P. acnes vis-a-vis AzA. Finally, ME hydrogel composite exhibited a better reduction in the papule density (93.75 ± 1.64%) in comparison to Aziderm™ 72.69 ± 4.67%) on acne as developed in rats by inducing testosterone. Thus, the developed AzA-TTO ME hydrogel composite promises an efficacious and comparatively safer drug delivery system for the topical therapy of acne vulgaris.
KW - Acne Vulgaris/chemically induced
KW - Animals
KW - Dicarboxylic Acids
KW - Hydrogels/therapeutic use
KW - Propionibacterium
KW - Rats
KW - Rats, Wistar
KW - Tea
KW - Tea Tree Oil
KW - Testosterone/therapeutic use
KW - Trees
U2 - 10.1007/s13346-021-01092-4
DO - 10.1007/s13346-021-01092-4
M3 - Article
C2 - 34782995
SN - 2190-393X
VL - 12
SP - 2501
EP - 2517
JO - Drug Delivery and Translational Research
JF - Drug Delivery and Translational Research
IS - 10
ER -