Liposomal-Based Formulations: A Path from Basic Research to Temozolomide Delivery Inside Glioblastoma Tissue

Amarandi, Roxana-Maria; Ibanescu, Alina; Carasevici, E; Marin, Luminița; Drăgoi, Brînduşa

doi:10.3390/pharmaceutics14020308

Cited by 26 publications

(17 citation statements)

References 173 publications

(235 reference statements)

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“…Liposomes are sphere-shaped vesicles of small diameter, ranging from a few nanometres to several micrometres, consisting of aqueous compartments surrounded by one or more lipid bilayers ( Figure 2 ) [ 25 ].…”

Section: Vesiclesmentioning

confidence: 99%

Erythromycin Formulations—A Journey to Advanced Drug Delivery

2022

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Erythromycin (ERY) is a macrolide compound with a broad antimicrobial spectrum which is currently being used to treat a large number of bacterial infections affecting the skin, respiratory tract, intestines, bones and other systems, proving great value from a clinical point of view. It became popular immediately after its discovery in 1952, due to its therapeutic effect against pathogens resistant to other drugs. Despite this major advantage, ERY exhibits several drawbacks, raising serious clinical challenges. Among them, the very low solubility in water and instability under acidic conditions cause a limited efficacy and bioavailability. Apart from this, higher doses promote drug resistance and undesirable effects. In order to overcome these disadvantages, during the past decades, a large variety of ERY formulations, including nanoparticles, have emerged. Despite the interest in ERY-(nano)formulations, a review on them is lacking. Therefore, this work was aimed at reviewing all efforts made to encapsulate ERY in formulations of various chemical compositions, sizes and morphologies. In addition, their preparation/synthesis, physico-chemical properties and performances were carefully analysed. Limitations of these studies, particularly the quantification of ERY, are discussed as well.

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Section: Vesiclesmentioning

confidence: 99%

Erythromycin Formulations—A Journey to Advanced Drug Delivery

2022

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“…The physicochemical characteristics of liposomes affect the degree of absorption of drugs and the nature of their release. The pharmacological activity of these nanotransporters also depends on their surface charge: the cationic surfaces of liposomes easily interact with anionic charged cell membranes due to greater affinity [ 53 , 60 , 61 ]. This leads to the accumulation of the drug and positive protons in the lysosomes of cells, their acidification and further lysis with the release of lysosomal content [ 62 , 63 , 64 ].…”

Section: Nanoscale Delivery Systemsmentioning

confidence: 99%

Temozolomide Efficacy and Metabolism: The Implicit Relevance of Nanoscale Delivery Systems

et al. 2022

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The most common primary malignant brain tumors in adults are gliomas. Glioblastoma is the most prevalent and aggressive tumor subtype of glioma. Current standards for the treatment of glioblastoma include a combination of surgical, radiation, and drug therapy methods. The drug therapy currently includes temozolomide (TMZ), an alkylating agent, and bevacizumab, a recombinant monoclonal IgG1 antibody that selectively binds to and inhibits the biological activity of vascular endothelial growth factor. Supplementation of glioblastoma radiation therapy with TMZ increased patient survival from 12.1 to 14.6 months. The specificity of TMZ effect on brain tumors is largely determined by special aspects of its pharmacokinetics. TMZ is an orally bioavailable prodrug, which is well absorbed from the gastrointestinal tract and is converted to its active alkylating metabolite 5-(3-methyl triazen-1-yl)imidazole-4-carbozamide (MTIC) spontaneously in physiological condition that does not require hepatic involvement. MTIC produced in the plasma is not able to cross the BBB and is formed locally in the brain. A promising way to increase the effectiveness of TMZ chemotherapy for glioblastoma is to prevent its hydrolysis in peripheral tissues and thereby increase the drug concentration in the brain that nanoscale delivery systems can provide. The review discusses possible ways to increase the efficacy of TMZ using nanocarriers.

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“…Liposomes have a significant perspective in cancer therapy because by targeting the active site, they do not damage the surrounding healthy tissue and thus give fewer side effects. To some extent, there are also yet unexplored application possibilities for liposomes, such as therapy for Alzheimer's disease [15,16].…”

Section: Applicationmentioning

confidence: 99%

Benefits of liposomal nonsteroid-anti-inflammatory drugs

Marković¹,

Kastratović²,

Nakarada³

et al. 2022

Hosp Pharm Int Multi J

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Introduction: Liposomes are small, spherical artificial vesicles that can be created from cholesterol and natural non-toxic phospholipids. Due to their size, hydrophobic and hydrophilic character (besides biocompatibility), liposomes are promising drug delivery systems. Topic: Liposomal formulations of non-steroidal anti-inflammatory drugs (NSAIDs) can be used in all population groups (children, adults, and the elderly) which gives them a wide range of applications. NSAIDs oral administration is associated with severe adverse effects in the gastrointestinal tract such as epigastric pain, heartburn, nausea, diarrhea, vomiting, peptic ulcer, and hepatic impairment. It has been observed in clinical trials, that liposomal formulations enhanced the drug permeability and the percentage of accumulated dose in the skin compared to control conventional gel formulations. Liposomal gel controls ibuprofen release and drug permeability in vitro and has shown a permeability pattern conducive to maintaining constant drug levels. Application: So far, liposomes containing sodium diclofenac, indomethacin, aceclofenac, and related NSAIDs have been produced in laboratory conditions. Liposomal technology is most commonly applied in cosmetology, cancer therapy and yet unexplored application possibilities for liposomes, such as therapy for Alzheimer's disease. Although varying in size and structure, they all possess certain common advantages - increased dermal availability of lipophilic drugs and their targeted delivery onto the required location. Liposomes have been proven highly effective in terms of retaining the NSAIDs in the synovial cavity, mostly because of their size and chemical composition. Undesirable therapy effects, fast clearance, and exposure to nontargeted sites could be minimized by administering NSAIDs using liposomes as carriers. Side effects and complications associated with the long-term oral and intramuscular applications of NSAIDs could especially be avoided using their liposomal formulations. Liposomes can be seen as ideal carriers for anti-inflammatory drugs as their ability to (passively) target sites of inflammation and release their content to inflammatory target cells enables them to increase local efficacy with only limited systemic exposure and adverse effects, improving bioavailability and patient compliance. A few NSAIDs are experimentally formulated in liposomes having improved pharmacokinetic characteristics. Further clinical investigations will show their pharmaco-dynamic effects. The in vitro release and ex vivo permeation (permeability) study showed a prolonged diclofenac release with high permeation flux. Conclusion: The use of liposomes as drug carriers becomes a notable positive step in the treatment of inflammatory, pain-causing, and rheumatic diseases. Liposomes present an attractive delivery system due to their flexible physicochemical and biophysical properties, which allow easy manipulation to address the different delivery considerations. The main objectives for the development of NSAIDs in liposomal carriers are deeper penetration of the active substance, fewer side effects, better and longer effect, the ability to change the characteristics of both the drug and the carrier, and adequate dose adjustment. Despite several challenges that accordingly still need to be addressed, liposomal drug formulations have significant health-promoting potential. Despite the encouragement of NSAID development and research studies, it still takes a long time for liposomal NSAID formulations to become available for everyday use.

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Liposomal-Based Formulations: A Path from Basic Research to Temozolomide Delivery Inside Glioblastoma Tissue

Cited by 26 publications

References 173 publications

Erythromycin Formulations—A Journey to Advanced Drug Delivery

Erythromycin Formulations—A Journey to Advanced Drug Delivery

Temozolomide Efficacy and Metabolism: The Implicit Relevance of Nanoscale Delivery Systems

Benefits of liposomal nonsteroid-anti-inflammatory drugs

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