Colloidal carriers for benzathine penicillin G: Nanoemulsions and nanocapsules

• Published in: International journal of pharmaceutics 2000-11, Vol.208 (1), p.71-80
• Main Authors: Santos-Magalhães, N.S, Pontes, A, Pereira, V.M.W, Caetano, M.N.P
• Format: Article
• Language: English
• Subjects: Antibacterial agents; Antibiotics. Antiinfectious agents. Antiparasitic agents; Benzathine penicillin G; Biological and medical sciences; Capsules; Chemistry, Pharmaceutical; Colloids; Drug Carriers; Emulsions; General pharmacology; In vitro release kinetic; Lactic Acid - chemistry; Lactic Acid - pharmacokinetics; Medical sciences; Nanocapsules; Nanoemulsions; Penicillin G Benzathine - chemistry; Penicillin G Benzathine - pharmacokinetics; Penicillins - chemistry; Penicillins - pharmacokinetics; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; PLGA poly ( d, l-lactic acid-co-glycolic acid) polymer; Polyglycolic Acid - chemistry; Polyglycolic Acid - pharmacokinetics; Polylactic Acid-Polyglycolic Acid Copolymer; Polymers - chemistry; Polymers - pharmacokinetics
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/S0378-5173(00)00546-9

The main purpose of this work is to formulate benzathine penicillin G nanoemulsion and nanocapsules, to evaluate their physicochemical and stabilising characteristics, and to determine their antimicrobial activity and penicillin in vitro release kinetics. Nanoemulsions were produced by the spontaneous emulsification approach and nanocapsules of poly ( d, l-lactic acid-co-glycolic acid) polymer (PLGA) were prepared by the method of interfacial deposition of a pre-formed polymer. A 207±8 nm mean diameter nanoemulsion formulation maintained stability for more than 5 months at 4°C. Stable nanocapsules with 224±58 nm mean diameter were obtained, which remained stabilised over 120 days at 4°C. The penicillin encapsulation ratio in the nanocapsules was 85%. The in vitro release profiles indicated that penicillin released from the nanoemulsion was similar to the one observed from nanocapsules. However it can be clearly deduced from the in vitro kinetic analysis that the antibiotic cannot be protected in colloidal delivery systems. Nevertheless, stable formulations obtained in this investigation supply a potential dosage form to encapsulate more easily soluble drugs.