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Acid-base combination principles for preparation of anti-acne dissolving microneedles loaded with azelaic acid and matrine
- Source :
- European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 165
- Publication Year :
- 2021
-
Abstract
- To overcome the poor solubility, skin irritation, and low permeability of azelaic acid (AZA) existed on the marketed formulations, a co-drug principle via matrine (MAT) was adopted to prepare anti-acne dissolving microneedles (DMNs). The formula was optimized according to the solubility and antibacterial activity of novel ionic salt. The results indicated solubilization of AZA could be achieved at a molar ratio between AZA and MAT was 1:1. Meanwhile, synergistic antibacterial and anti-irritative properties were acquired. The matrix materials were composed of sodium carboxymethyl cellulose (CMC), polyvinylpyrrolidone (PVP), and trehalose. And drug loadings of AZA and MAT in DMNs were 201.88 ± 4.81 µg and 259.71 ± 1.72 µg, respectively. After insertion into porcine skin for 10 h, the cumulative permeability of AZA and MAT were 68.16% ± 3.79% and 57.37 ± 5.17%, respectively, while just 4.13 ± 0.39% (p < 0.01) was detected for commercially available AZA gel. In vitro antibacterial experiment, bacteriostatic rates of DMNs were all above 95% for Staphylococcus aureus, Staphylococcus epidermidis, and Propionibacterium acnes. Besides, DMNs exhibited no cytotoxicity and skin irritation. In conclusion, combination between AZA and MAT addressed shortcomings of AZA, and made it easier, safer, and more effective in acne treatment.
- Subjects :
- Azelaic acid
Swine
Pharmaceutical Science
medicine.disease_cause
Administration, Cutaneous
chemistry.chemical_compound
Alkaloids
Matrine
Staphylococcus epidermidis
Acne Vulgaris
medicine
Animals
Dicarboxylic Acids
Solubility
Matrines
Skin
Polyvinylpyrrolidone
biology
Chemistry
biology.organism_classification
Carboxymethyl cellulose
Staphylococcus aureus
Antibacterial activity
Quinolizines
medicine.drug
Nuclear chemistry
Subjects
Details
- ISSN :
- 18790720
- Volume :
- 165
- Database :
- OpenAIRE
- Journal :
- European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
- Accession number :
- edsair.doi.dedup.....112191ba4f285febf41926b83849775d