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Liposomal encapsulation of chemotherapeutic agents

Cancer is the second-leading cause of mortality worldwide, and the number of annual deaths continues to rise. From 2005 to 2015, for instance, cancer cases rose by 33 percent in a majority of countries. While some of this troubling increase may be attributed to overall growth in population and aging, it’s clear that the need has never been greater for effective chemotherapy drugs and other cancer therapies.

Fortunately, medical science has not been idle. Modern oncology has more tools in its arsenal — many of them featuring enhanced efficacy and reduced side effects — than ever before. Despite noting that cancer incidence is expected to continue to increase for the foreseeable future, hope is not lost: “… Progress is possible in the war against cancer,” wrote the authors of the Global Burden of Disease Cancer Collaboration.

Liposome Nanocarriers For Cancer Treatment

Some of this optimism reflects excitement over the growing use of nanocarriers, such as liposomes. First described in the mid-1960s and pioneered in the late 1980s, this still-emerging technology utilizes liposomal microencapsulation of chemotherapy drugs to enhance efficacy. By enrobing cytotoxins in liposomes comprised of phospholipid bilayers, it’s possible to dramatically improve efficacy in many instances, while simultaneously reducing unintended side effects. What’s more, these tiny drug-delivery packages offer better bioavailability, while being biocompatible and biodegradable.

Of course, cancer chemotherapy is notorious for yielding noxious side effects that diminish the patient's quality of life, while significantly boosting the threat of patient noncompliance due to tolerability concerns. Chemotherapy drugs are invariably highly cytotoxic. While they ideally target fast-replicating cancer cells selectively, these drugs are also capable of doing serious harm to healthy “bystander” cells.

By encapsulating cytotoxins in liposomes, these risky drugs can be delivered more safely and effectively to their intended targets, while largely sparing healthy tissues. Microencapsulation helps prevent drug degradation, and liposome technology offers the flexibility to incorporate both hydrophilic and hydrophobic compounds. The vanishingly small sizes of these liposome drug-delivery vessels mean they are readily incorporated into target tissues. Thus, this advanced technology has overcome some of the most glaring limitations of conventional chemotherapy.

Enhanced Efficacy of Liposome Drug Delivery Reduces Side Effects

Depending on the process, equipment and lipids used, it’s possible to tailor the characteristics of a given liposome to suit specific needs. Size, charge, composition and other characteristics can all affect the in-vivo performance of the liposome. For example, the common breast cancer antineoplastic agent doxorubicin has been successfully encapsulated since the turn of the century.

The use of liposomal doxorubicin has greatly reduced its cardiotoxicity among countless subsequent patients. Doxorubicin chemotherapy represents an important tool in the oncologist’s arsenal, which has been used to treat breast cancer and other forms of cancer for decades. While their mother’s generation often died from heart disease after receiving nominally successful treatment for breast cancer, today’s patients can expect to avoid this particular, potentially deadly side effect of chemotherapy. Similarly, encapsulation of the common breast cancer agent, paclitaxel, has dramatically reduced its neurotoxicity.

As noted in an ONCOLOGY article, “Liposomal encapsulation of doxorubicin significantly alters its pharmacokinetic profile, attenuates its toxicity patterns in clinical settings, and demonstrates in preclinical trials an ability to reverse multi-drug resistance.” The latter benefit refers to yet another advantage of microencapsulation: It helps limit the development of resistance by cancer cells to the antineoplastic activity of a given chemotherapeutic agent.

Microfluidics Technology For Cancer Therapy

Competing in today’s high-stakes pharmaceutical arena means possessing the capability to investigate, develop and produce drugs quickly, safely and efficiently.

At Microfluidics, we have the right equipment to help you meet your R&D, pilot and production goals. We specialize in engineering, manufacturing and servicing robust machinery that readily produces pharmaceutical-grade liposomes. Achieve consistent particle size reductions; combined with tighter particle size distributions, invest in liposome technology, perform nanoencapsulation and more by leveraging industry-leading pharmaceutical manufacturing technology — available only from Microfluidics.

Contact us today for more information about how our Microfluidizer® high shear fluid processors and high-pressure homogenizers can benefit your bottom line.

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Posted by Steve Mesite
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