Abstract:
:Local anaesthetics may be added to intravenous o/w emulsions of propofol to reduce the initial pain of injection. Due to incompatibility problems of the emulsion on the addition of a local anaesthetic solution, prior encapsulation of the drug within liposomes is suggested. The liposomes were prepared with the sonication method and loaded with either lidocaine hydrochloride (LiHCl) or prilocaine hydrochloride (PrHCl). The liposomal systems were characterised with photon correlation spectroscopy (PCS) in terms of mean particle size and polydispersity. Lamellarity and lamellar thickness were determined by small angle X-ray scattering (SAXS). Visualisation of drug-loaded liposomes was performed with transmission electron microscopy (TEM) after freeze fracture replication of the samples. Depending on the manufacturing procedure mean particle sizes of the drug-free liposomes varied from 150 +/- 9 nm to 102 +/- 2 nm. Drug-loaded liposomes manufactured the same way showed reduced particle sizes of 125 +/- 1 nm and 85 +/- 7 nm, respectively. Determination of bilayer thickness by SAXS yielded 6.2 +/- 0.2 nm in the case of full hydration whereas the bilayer thickness without the hydration shell was just 4.4 +/- 0.2 nm. The small particle sizes achieved are appropriate for intravenous administration.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Müller M,Mackeben S,Müller-Goymann CCdoi
10.1016/j.ijpharm.2004.01.015keywords:
subject
Has Abstractpub_date
2004-04-15 00:00:00pages
139-48issue
1-2eissn
0378-5173issn
1873-3476pii
S0378517304000304journal_volume
274pub_type
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