Transdermal absorption of clindamycin and tretinoin from topically applied anti‐acne formulations in man

Abstract

ABSTRACT:The percutaneous absorption of clindamycin was studied in healthy male volunteers, comparing two investigative clindamycin (% w/v)/tretinoin (0.025% w/v) gels, containing clindamycin phosphate ester and clindamycin HCl, respectively, relative to a clindamycin phosphate lotion (1% clindamycin; Dalacin T ® ). Formulations were applied daily for 5 days on the face, according to a balanced complete block design. Redness of the skin was scored visually, and blood and urine were collected. Clindamycin plasma levels did not exceed the limit of quantification (5 ng mL − 1 ) with the clindamycin phosphate formulations, but one volunteer who received the clindamycin HCl/tretinoin gel showed plasma levels of up to 13 ng mL − 1 . Clindamycin urinary excretion for 12 h after application of the clindamycin phosphate/tretinoin gel was comparable to the values of the reference lotion, whereas the clindamycin HCl/tretinoin gel gave significantly higher values. Erythema appeared to be associated with increased urinary excretion. The formulations were tolerated well. In a separate clinical pilot study in acne patients, the transdermal uptake of tretinoin and clindamycin from the clindamycin phosphate/tretinoin gel was monitored. Plasma samples were collected after 4 and 12 weeks of daily treatment. None of the study plasma samples contained measurable tretinoin levels. Clindamycin levels were not quantifiable in the majority (87%) of samples, the highest plasma level was 11 ng mL. The chemical form of clindamycin proved to modulate skin irritation and percutaneous uptake of clindamycin from a gel formulation in healthy subjects. There was no indications for a notable transdermal uptake of tretinoin during daily application of the gel in patients, nor for an enhancing effect of tretinoin on clindamycin uptake.

Topical clindamycin in the management of acne vulgaris

“……”

Simultaneous Analysis of Multiple Classes of Antibiotics by Ion Trap LC/MS/MS for Assessing Surface Water and Groundwater Contamination

“…Surface water from a second location on the Niagara River revealed clindamycin at a concentration of 1.1 µg/L. Clindamycin is a lincosamide antibiotic often used in the topical treatment of acne 32 and has been detected in surface waters. 33 Wastewater effluents from East Aurora and Holland, NY, exhibited caffeine and several antibiotic concentrations, ranging from 0.10 to 1.3 µg/L and are listed in Table 6.…”

“…Surface water from a second location on the Niagara River revealed clindamycin at a concentration of 1.1 μg/L. Clindamycin is a lincosamide antibiotic often used in the topical treatment of acne and has been detected in surface waters .…”

Treatment of Acne Vulgaris During Pregnancy and Lactation: A Narrative Review

“…While there are limited data on sodium sulfacetamide safety, no fetal anomalies have been reported, and it is likely safe during all phases of pregnancy [6,21,[35][36][37]. Given minimal systemic absorption, there is low concern for appreciable folic acid reduction in pregnant patients [6,17,33].…”

“…Topical Clindamycin Topical clindamycin is the most prescribed topical antibiotic for acne. Although studies are limited, topical clindamycin is known to cause negligible systemic absorption and is considered safe during all trimesters of pregnancy and lactation [6,11,15,17,21,22,37]. In general, oral drugs deemed safe during pregnancy and lactation, including clindamycin, are also safe in topical forms [6].…”