Solid Lipid Nanoparticles Loaded with Retinoic Acid and Lauric Acid as an Alternative for Topical Treatment of Acne Vulgaris.
Topical therapy is the first choice for the treatment of mild to moderate acne and all-trans retinoic acid is one of the most used drugs. The combination of retinoids and antimicrobials is an innovative approach for acne therapy. Recently, lauric acid, a saturated fatty acid, has shown strong antimicrobial activity against Propionibacterium acnes. However, topical application of retinoic acid is followed by high incidence of side-effects, including erythema and irritation. Solid lipid nanoparticles represent an alternative to overcome these side-effects. This work aims to develop solid lipid nanoparticles loaded with retinoic acid and lauric acid and evaluate their antibacterial activity. The influence of lipophilic stearylamine on the characteristics of solid lipid nanoparticles was investigated. Solid lipid nanoparticles were characterized for size, zeta potential, encapsulation efficiency, differential scanning calorimetry and X-ray diffraction. The in vitro inhibitory activity of retinoic acid-lauric acid-loaded solid lipid nanoparticles was evaluated against Propionibacterium acnes, Staphylococcus aureus and Staphylococcus epidermidis. High encapsulation efficiency was obtained at initial time (94 ± 7% and 100 ± 4% for retinoic acid and lauric acid, respectively) and it was demonstrated that lauric acid-loaded-solid lipid nanoparticles provided the incorporation of retinoic acid. However, the presence of stearylamine is necessary to ensure stability of encapsulation. Moreover, retinoic acid-lauric acid-loaded solid lipid nanoparticles showed growth inhibitory activity against Staphylococcus epidermidis, Propionibacterium acnes and Staphylococcus aureus, representing an interesting alternative for the topical therapy of acne vulgaris.
Elton Luiz
EL
Silva
Guilherme
G
Carneiro
Lidiane Advíncula
LA
De Araújo
Mariana de Jesus Vaz
Mde J
Trindade
Maria Irene
MI
Yoshida
Rodrigo Lambert
RL
Oréfice
Luis de Macêdo
Lde M
Farias
Maria Auxiliadora Roque
MA
De Carvalho
Simone Gonçalves
SG
Dos Santos
Gisele Assis Castro
GA
Goulart
Ricardo José
RJ
Alves
Lucas Antônio Miranda
LA
Ferreira
D000152:Acne Vulgaris; D000287:Administration, Topical; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D004355:Drug Stability; D007850:Lauric Acids / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011425:Propionibacterium acnes / Q000187:drug effects; D013210:Staphylococcus / Q000187:drug effects; D014212:Tretinoin / Q000737:chemistry / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D007850:Lauric Acids; C030358:lauric acid; D014212:Tretinoin