Gentamicin (GM) is an important aminoglycoside antibiotic for the treatment of infections caused by a wide spectrum of aerobic gram-negative bacilli and gram-positive cocci. As a class, the aminoglycosides are poorly absorbed from the gastrointestinal (GI) tract and are commonly used as injectable and topical preparations. This study was aimed at finding the effect of a novel emulsifier, Labrasol, on the absorption of GM from the GI tract of rats. GM formulations were prepared, either as saline solution or as Labrasol microemulsions, and were administrated to rat small intestine and colon. Plasma GM levels following intestinal application were compared to those obtained with intravenous (i.v.) administration. A 5 mg/kg dose of GM preparation containing Labrasol, 1 ml/kg, administrated into colon resulted in the mean AUC of 21.179+/-1.374 microg x h/ml, compared to 7.813+/-0.105 microg x h /ml obtained with i.v. administration of GM, 1 mg/kg. The absolute bioavailability (BA) of the Labrasol preparation was 54.2%. Labrasol facilitates the transmucosal delivery of GM from rat colon by forming microemulsions, and the BA obtained with Labrasol microemulsion was higher than with other surfactants (8.4% for Tween 80 and 3.4% for Transcutol P). Additionally, in vitro permeation studies demonstrated that Labrasol also inhibited the intestinal secretory transport. The effect of Labrasol is ascribed to both (1) enhanced GM absorption from the GI lumen into the systemic circulation and (2) inhibition of efflux of GM from the enterocytes to the GI lumen.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/s0024-3205(01)01375-3 | DOI Listing |
J Chromatogr A
January 2025
Laboratory of Pharmaceutics and Nanotechnology (LDGNano), School of Pharmacy, Federal University of Ouro Preto, Minas Gerais 35400-000, Brazil. Electronic address:
Chagas disease is the major cause of death by cardiomyopathy in Latin America. Benznidazole (BZN) tablets are the standard of care for Chagas disease, and recently, self-emulsifying systems (SEDDS) have shown promising efficacy as the BZN delivery system, particularly for pediatric use. However, the comparative effects of surfactants on the physicochemical properties of SEDDS have been poorly investigated to date.
View Article and Find Full Text PDFJ Cosmet Dermatol
November 2024
Clinical Research Development Centre, Imam Hossein Educational Hospital, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Background: Valproic acid (VPA) is used to treat various neurological and psychiatric conditions. While oral VPA can cause hair loss, topical application has shown potential for hair regeneration. This study aimed to develop and evaluate microemulsion (ME) formulations of VPA for enhanced transfollicular delivery.
View Article and Find Full Text PDFArch Pharm (Weinheim)
January 2025
Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, India.
Pazopanib hydrochloride (PZH) is a Biopharmaceutics Classification System class II drug that faces challenges at the formulation forefront including low aqueous solubility (0.043 mg/mL) and poor oral bioavailability (14-39%). The present investigation aimed to develop a self-microemulsifying drug delivery system (SMEDDS) of PZH using a blend of Capryol® 90, Labrasol®, and propylene glycol to improve its solubility.
View Article and Find Full Text PDFNaunyn Schmiedebergs Arch Pharmacol
September 2024
Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, V.L. Mehta Road, Vile Parle (W), Mumbai, 400056, Maharashtra, India.
Int J Pharm
November 2024
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!