New aspects of controlled release systems for local anaesthetics: A review

Formulation and optimisation of novel transfersomes for sustained release of local anaesthetic

“…Transfersome samples that were prepared by EPC not only showed sustained release of lidocaine but also a delayed release, with <2% drug released after 1 h (F2, F5, and F8), but subsequently almost 60% after 3 h (Table ). DMPC‐based transfersomes showed between 5% and 21% drug release after 1 h. The release profiles of the six formulations proved that transfersomes were successfully optimised and prepared to sustain the release lidocaine over 24 h. Moreover, it is a promising system to deliver LA via any route with a reduced frequency of administration, which in turn would reduce side effects and enhance the pain management (both acute and chronic) …”

“…The prolonged effect is mainly gained by either the addition of a vasoconstrictor e.g. epinephrine, which prevents the leakage of the LA to the blood stream, or through liposomal and lipid‐based Depofoam formulations . To our knowledge, several attempts have been made to formulate LAs as polymeric or lipid‐based microspheres and nanoparticles for injectable or transdermal drug delivery.…”

“…[3,9,10] Local anaesthetics (LA) such as lidocaine, bupivacaine and ropivacaine block the transmission of painful stimuli to the brain by acting on ion channels of nociceptor fibres, to achieve a control for both acute and chronic pain. [11] In order to improve their pharmacokinetic properties, prolong their pharmacological activity and minimise their toxicity, many studies have formulated LAs in different forms such as injectable implants, films, microstructural systems, polymeric nanoparticles and lipid-based vesicles. [12,13] However, most of the available LA forms have short duration of action, and frequent application is required to get long-term pain relief which inversely affects the patient compliance and increases the side effects.…”

“…epinephrine, which prevents the leakage of the LA to the blood stream, or through liposomal and lipid-based Depofoam formulations. [16,17] To our knowledge, several attempts have been made to formulate LAs as polymeric or lipid-based microspheres and nanoparticles for injectable or transdermal drug delivery. However, most of the systems developed were not intended for sustained-release administration.…”

Development of Smart Polymer Microparticles through Suspension Polymerization for Treatment of Schistosomiasis

“…As reported in the literature, possible alternatives to overcome these problems are drug encapsulation and manufacture of controlled release systems . Among the many competitive advantages that can be obtained in these cases, one can cite the increase of drug absorption rates, attainment of more uniform drug concentrations in the body, reduction of the amounts required for drug administration, improvement of patient compliance, and reduction of treatment costs …”