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Introduction
Contents:
  1. Optimization Strategies
  2. Targeting of Drugs 2
  3. [Full text] Recent expansions of novel strategies towards the drug targeting into | IJN
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Structures of Different Liposomal Preparations A Classical liposome encapsulating lipid soluble drugs; B classical liposome encapsulating aqueous soluble drugs; C sterically stabilized liposomes; D ligand-targeted liposome containing an aqueous soluble drug. World Scientific Publishing, Thermosensitive liposomal drug delivery systems: state of the art review. Nanomedicine , 9 , — Thermosensitive liposomes for localized delivery and triggered release of chemotherapy. On the formulation of pH-sensitive liposomes with long circulation times.

A Classical liposome encapsulating lipid soluble drugs; B classical liposome encapsulating aqueous soluble drugs; C sterically stabilized liposomes; D ligand-targeted liposome containing an aqueous soluble drug. Liposomal nanomedicines. Handbook of Nanobiomedical Research. Torchilin V ed. Several recent reports have discussed specific aspects of liposomes regarding novel structural formulations or current clinical progress.

Optimization Strategies

In this review, we highlight some inherent liposomal problems facing their optimized design. We also place special focus on recent applications of liposomes as efficient delivery systems. Drug loading into nanoparticles, including liposomes, is known to increase the therapeutic ratio of the entrapped drug by permitting selective delivery of adequate concentrations of the entrapped drug to the site of action while restraining its delivery to non-target normal tissues.

Encapsulation in a rapid-release liposomal formulation enhances the anti-tumor efficacy of pemetrexed in a murine solid mesothelioma-xenograft model.

Targeting of Drugs 2

Anti-CDtargeted liposomal doxorubicin improves the therapeutic efficacy in murine B-cell lymphoma and ameliorates the toxicity of liposomes with varying drug release rates. Cancer Res. Active methods of drug loading into liposomes: recent strategies for stable drug entrapment and increased in vivo activity. Expert Opin. Transmembrane ammonium sulfate gradients in liposomes produce efficient and stable entrapment of amphipathic weak bases.

[Full text] Recent expansions of novel strategies towards the drug targeting into | IJN

Although the above strategy has proven advantageous in certain circumstances, active loading is not considered a universal method with many drugs that are highly hydrophobic or lack an ionizable group, such as paclitaxel or ciprofloxacin, which cannot be remotely loaded into liposomes. In vitro and in vivo antitumoral activity of free, and encapsulated taxol.

Remote loading of preencapsulated drugs into stealth liposomes. Novel tretinoin formulations: a drug-in-cyclodextrin-in-liposome approach. Liposome Res. Enhanced active liposomal loading of a poorly soluble ionizable drug using supersaturated drug solutions. It is well recognized that the entrapped drug within liposomes is not bioavailable until it is released. Liposomal drug delivery systems: from concept to clinical applications.

Determination of doxorubicin levels in whole tumor and tumor nuclei in murine breast cancer tumors. Optimization of the retention properties of vincristine in liposomal systems. Lung Cancer , 34 , — Advanced therapeutic approach for the treatment of malignant pleural mesothelioma via the intrapleural administration of liposomal pemetrexed. Release , Pt A , 29—36 Drug release from liposomes was demonstrated influenced by liposomal membrane composition and the physicochemical properties of the encapsulated drug. Serum-induced leakage of liposome contents.

Factors affecting the encapsulation of drugs within liposomes. Liposomal pemetrexed: formulation, characterization and in vitro cytotoxicity studies for effective management of malignant pleural mesothelioma. Lateral diffusion rates of phosphatidylcholine in vesicle membranes: effects of cholesterol and hydrocarbon phase transitions. Influence of lipid composition on the antitumor activity exerted by doxorubicin-containing liposomes in a rat solid tumor model. Spin label partitioning in lipid vesicles.

A model study for drug encapsulation. Acta , , 57—68 Characterization of liposomal systems containing doxorubicin entrapped in response to pH gradients.

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Liposome-encapsulated vincristine, vinblastine and vinorelbine: a comparative study of drug loading and retention. Except for the treatment of diseases where there was an MPS involvement, e. Therapy of leishmaniasis: superior efficacies of liposome-encapsulated drugs. Stealth liposomes: review of the basic science, rationale, and clinical applications, existing and potential. Nanomedicine , 1 , — Uptake of liposomes by cultured mouse bone marrow macrophages: influence of liposome composition and size. Acta , , 56—64 Influence of dose on liposome clearance: critical role of blood proteins.

Acta , , 31—37 Association of blood proteins with large unilamellar liposomes in vivo.

Relation to circulation lifetimes. Fate and behavior of liposomes in vivo : a review of controlling factors.


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Drug Carrier Syst. Scavenger receptor-mediated uptake and metabolism of lipid vesicles containing acidic phospholipids by mouse peritoneal macrophages. Transfer and exchange of phospholipid between small unilamellar liposomes and rat plasma high density lipoproteins. Dependence on cholesterol content and phospholipid composition.

Liposomal blockade of the reticuloendothelial system: improved tumor imaging with small unilamellar vesicles. Science , , — Liposome disposition in vivo : effects of pre-dosing with lipsomes. Large unilamellar liposomes with low uptake into the reticuloendothelial system. Amphipathic polyethyleneglycols effectively prolong the circulation time of liposomes. Release , 74 , 47—61 Pegylated liposomal doxorubicin: metamorphosis of an old drug into a new form of chemotherapy. Cancer Invest. The lipophilic nature of the biological membranes restricts direct entrance of liposomes into target cells.

Powering membrane traffic in endocytosis and recycling. Cell Biol. Recent approaches to intracellular delivery of drugs and DNA and organelle targeting. Design and evaluation of pH-sensitive liposomes constructed by poly 2-ethyloxazoline -cholesterol hemisuccinate for doxorubicin delivery. Delivery of macromolecules using arginine-rich cell-penetrating peptides: ways to overcome endosomal entrapment. AAPS J.

Lecture 3 Target and Lead Identification

Cell-penetrating peptide induces leaky fusion of liposomes containing late endosome-specific anionic lipid. Liposomes have demonstrated a wide range of applications in clinical settings. These applications ranged from therapeutic and diagnostic to, most recently, theranostic applications Fig.

Delivery of small molecule therapeutics, particularly chemotherapeutic agents, was one of the first clinical applications of liposomal delivery systems. The distribution of the anticancer drug doxorubicin in relation to blood vessels in solid tumors. Prevention of chronic doxorubicin cardiotoxicity in beagles by liposomal encapsulation. Liposomal doxorubicin: antitumor activity and unique toxicities during two complementary phase I studies.

Despite the aforementioned advances achieved by passive targeting-mediated delivery of liposomal anticancer drugs, many reports have emphasized the failure of such targeting strategy in ensuring the adequate delivery of a minimum therapeutic concentration of encapsulated drug within tumor tissue, resulting in treatment failure. A variety of molecules, including peptides, antibodies, proteins, charged molecules, and some low-molecular weight ligands, such as folate, and nucleic acid-based aptamers, have been studied in conjunction with liposomes for enhanced anticancer treatment.

Folate-mediated tumor cell targeting of liposome-entrapped doxorubicin in vitro. Peptide ligand-mediated liposome distribution and targeting to EGFR expressing tumor in vivo. Matrix metalloprotease 2-responsive multifunctional liposomal nanocarrier for enhanced tumor targeting. ACS Nano , 6 , — Targeted delivery of methotrexate to skeletal muscular tissue by thermosensitive magnetoliposomes. Locoregional cancer treatment with magnetic drug targeting. A new temperature-sensitive liposome for use with mild hyperthermia: characterization and testing in a human tumor xenograft model.

Ultrasound triggered release of cisplatin from liposomes in murine tumors. Release , , 63—68 In addition to cancer chemotherapy, liposomal delivery systems have been used for the treatment of other diseases.