Liposomski antibiotici

master's thesis

• Title (english): Liposomal antibiotics
• Author: Antonela Buljan
• Mentor: Željka Vanić (mentor)
• Committee member: Željka Vanić (predsjednik povjerenstva)
• Committee member: Mario Jug (član povjerenstva)
• Committee member: Sanda Vladimir-Knežević (član povjerenstva)
• Granter: University of Zagreb; Faculty of Pharmacy and Biochemistry; (Department of pharmaceutical technology); Zagreb
• Defense date and country: 2021-07-16, Croatia
• Scientific / art field, discipline and subdiscipline: BIOMEDICINE AND HEALTHCARE; Pharmacy; Pharmacy

Abstract

Antimikrobna rezistencija je tijekom zadnja dva desetljeća postala jedan od glavnih problema u učinkovitoj antimikrobnoj terapiji. Znanstvenici predlažu dva smjera u borbi protiv rezistencije: razvoj novih antibiotika ili unaprjeđenje postojećih uklapanjem u različite lipidne i polimerne nanosustave te hibridne sustave s antimikrobnim peptidima.
Uklapanjem antibiotika u liposome poboljšavaju se njegova farmakokinetička svojstva i bioraspoloživost, smanjuje toksičnost, te u većini slučajeva povećava antimikrobna aktivnost. Osim toga, liposomi služe kao zaštita antibiotika od neželjenih učinaka metabolizma, a pritom štite i pacijenta koji uzima lijek od neželjenih nuspojava antibiotika. Liposomski antibiotici mogu biti dizajnirani da ciljaju intracelularne infekcije gdje važnu ulogu imaju konvencionalni liposomi koji bivaju fagocitirani i transportirani do inficiranih stanica. PEG-iliranjem površine liposoma produljuje se vrijeme polueliminacije što doprinosi održavanju konstantne razine antibiotika u serumu. Liposomi koji na svojoj površini imaju imunoglobuline, proteine ili saharide usmjereni su prema specifičnim ciljevima kao što su određena tkiva, patogeni ili bakterijski biofilm.
Brojna istraživanja u ovom području rezultirala su kliničkim ispitivanjima liposomskih antibiotika, a neki od njih su i registrirani, što je sistematizirano prikazano ovim radom.

Abstract (english)

Antimicrobial resistance has become one of the major problem for effective antimicrobial therapy, and the list of antibiotic-resistant bacteria is increasing over the last two decades. To overcome this problem, scientists suggest two options: the development of new antibiotics or the improvement of already existing antibiotics by their incorporation in nanocarriers and synthesis of antimicrobial peptides. Among the various nanosystems investigated, liposomes have the longest clinical use.
Incorporation of antibiotics into liposomes results in: improved pharmacokinetics and bioavailability of the liposomally-incorporated antibiotic, reduced toxicity, increased activity against intracellular and extracellular pathogens and modified drug release. Liposomes serve as a way of protecting antibiotics against early metabolic degradation, as well as protecting patients against drug side effects. Liposomal antibiotics can be ingested by macrophages and transported to the infected cells. By modifying the liposomal surface by polyetileneglycol derivatives, the circulation time increases, thus mantaining adequate levels of the antibiotic in serum. Moreover, to achieve targeted delivery to pathogens and biofilm, the liposomal surface can be modified with immunoglobulins, proteins or saccharides.
This paper provides an overview of selected, the most perspective, liposomal antibiotics aimed for parenteral, pulmonary and dermal delivery, which are currently in preclinical and clinical studies.

• Keywords: antimikrobna rezistencija; liposomi; novi antibiotici; nanosustavi; parenteralni liposomi; topikalni liposomi; inhalacijski liposomi
• Keywords (english): antimicrobial resistance; liposomes; new antibiotics; nanocarriers; parenteral liposomes; topical liposomes; mupirocin; arikace; inhaled liposomal antibiotic; pulmonary liposomes
• Language: croatian
• URN:NBN: urn:nbn:hr:163:482528
• Study programme: Title: Pharmacy; Study programme type: university; Study level: integrated undergraduate and graduate; Academic / professional title: magistar/magistra farmacije (magistar/magistra farmacije)
• Type of resource: Text
• File origin: Born digital
• Access conditions: Open access; Embargo expiration date: 2023-07-16
• Created on: 2022-03-01 10:48:26