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      Liposomal Formulations in Clinical Use: An Updated Review

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          Abstract

          Liposomes are the first nano drug delivery systems that have been successfully translated into real-time clinical applications. These closed bilayer phospholipid vesicles have witnessed many technical advances in recent years since their first development in 1965. Delivery of therapeutics by liposomes alters their biodistribution profile, which further enhances the therapeutic index of various drugs. Extensive research is being carried out using these nano drug delivery systems in diverse areas including the delivery of anti-cancer, anti-fungal, anti-inflammatory drugs and therapeutic genes. The significant contribution of liposomes as drug delivery systems in the healthcare sector is known by many clinical products, e.g., Doxil ®, Ambisome ®, DepoDur™, etc. This review provides a detailed update on liposomal technologies e.g., DepoFoam™ Technology, Stealth technology, etc., the formulation aspects of clinically used products and ongoing clinical trials on liposomes.

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          Nanomedicine in cancer therapy: challenges, opportunities, and clinical applications.

          Andreas Wicki, Dominik Witzigmann, Vimalkumar Balasubramanian … (2015)
          Cancer is a leading cause of death worldwide. Currently available therapies are inadequate and spur demand for improved technologies. Rapid growth in nanotechnology towards the development of nanomedicine products holds great promise to improve therapeutic strategies against cancer. Nanomedicine products represent an opportunity to achieve sophisticated targeting strategies and multi-functionality. They can improve the pharmacokinetic and pharmacodynamic profiles of conventional therapeutics and may thus optimize the efficacy of existing anti-cancer compounds. In this review, we discuss state-of-the-art nanoparticles and targeted systems that have been investigated in clinical studies. We emphasize the challenges faced in using nanomedicine products and translating them from a preclinical level to the clinical setting. Additionally, we cover aspects of nanocarrier engineering that may open up new opportunities for nanomedicine products in the clinic.
          Article 0 comments Cited 490 times – based on 0 reviews     Review now
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            To exploit the tumor microenvironment: Since the EPR effect fails in the clinic, what is the future of nanomedicine?

            F Danhier (2016)
            Tumor targeting by nanomedicine-based therapeutics has emerged as a promising approach to overcome the lack of specificity of conventional chemotherapeutic agents and to provide clinicians the ability to overcome shortcomings of current cancer treatment. The major underlying mechanism of the design of nanomedicines was the Enhanced Permeability and Retention (EPR) effect, considered as the "royal gate" in the drug delivery field. However, after the publication of thousands of research papers, the verdict has been handed down: the EPR effect works in rodents but not in humans! Thus the basic rationale of the design and development of nanomedicines in cancer therapy is failing making it necessary to stop claiming efficacy gains via the EPR effect, while tumor targeting cannot be proved in the clinic. It is probably time to dethrone the EPR effect and to ask the question: what is the future of nanomedicines without the EPR effect? The aim of this review is to provide a general overview on (i) the current state of the EPR effect, (ii) the future of nanomedicine and (iii) the strategies of modulation of the tumor microenvironment to improve the delivery of nanomedicine.
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              Stealth liposomes: review of the basic science, rationale, and clinical applications, existing and potential

              Maria Laura Immordino, Franco Dosio, Luigi Cattel (2006)
              Among several promising new drug-delivery systems, liposomes represent an advanced technology to deliver active molecules to the site of action, and at present several formulations are in clinical use. Research on liposome technology has progressed from conventional vesicles (“first-generation liposomes”) to “second-generation liposomes”, in which long-circulating liposomes are obtained by modulating the lipid composition, size, and charge of the vesicle. Liposomes with modified surfaces have also been developed using several molecules, such as glycolipids or sialic acid. A significant step in the development of long-circulating liposomes came with inclusion of the synthetic polymer poly-(ethylene glycol) (PEG) in liposome composition. The presence of PEG on the surface of the liposomal carrier has been shown to extend blood-circulation time while reducing mononuclear phagocyte system uptake (stealth liposomes). This technology has resulted in a large number of liposome formulations encapsulating active molecules, with high target efficiency and activity. Further, by synthetic modification of the terminal PEG molecule, stealth liposomes can be actively targeted with monoclonal antibodies or ligands. This review focuses on stealth technology and summarizes pre-clinical and clinical data relating to the principal liposome formulations; it also discusses emerging trends of this promising technology.
              Article 0 comments Cited 324 times – based on 0 reviews     Review now
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                Author and article information

                Contributors
                Murali Mohan Yallapu: Role: Academic Editor
                Journal
                Journal ID (nlm-ta): Pharmaceutics
                Journal ID (iso-abbrev): Pharmaceutics
                Journal ID (publisher-id): pharmaceutics
                Title: Pharmaceutics
                Publisher: MDPI
                ISSN (Electronic): 1999-4923
                Publication date (Electronic): 27 March 2017
                Publication date Collection: June 2017
                Volume: 9
                Issue: 2
                Electronic Location Identifier: 12
                Affiliations
                Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Hyderabad 500037, India; upendra.bulbake@ 123456gmail.com (U.B.); dsdoppalapudisindhu@ 123456gmail.com (S.D.); nagavendra.kommineni@ 123456gmail.com (N.K.)
                Author notes
                [* ]Correspondence: wahid@ 123456niperhyd.ac.in
                [†]

                These authors contributed equally to this work.

                Article
                Publisher ID: pharmaceutics-09-00012
                DOI: 10.3390/pharmaceutics9020012
                PMC ID: 5489929
                PubMed ID: 28346375
                SO-VID: 05886427-e586-46a3-b768-e753ca627205
                Copyright © © 2017 by the authors.
                License:

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

                History
                Date received : 16 January 2017
                Date accepted : 23 March 2017
                Categories
                Subject: Review

                Keywords: liposomes,therapeutics,drug delivery,liposome technology,nanotechnology,clinical trials,marketed products
                Data availability:
                Keywords: liposomes, therapeutics, drug delivery, liposome technology, nanotechnology, clinical trials, marketed products

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