The emergence of Nanoparticles in Pharmaceuticals & Healthcare Industry

Nanoparticles in pharmaceuticals and healthcare

Nanoparticles with its unique features are revolutionizing almost every type of industry. It varies in size but generally ranges from 100 nm to 500 nm. Nanomedicine is the application of nanoparticles in pharmaceuticals and healthcare sectors. Nanoparticles can be manipulated in terms of size, surface characteristics, and material used. As a result of the manipulation of nanoparticles, it can be developed into smart systems encasing therapeutic, imaging agents that can be readily employed in pharmaceuticals and healthcare units. Nanomedicines are highly targeting specific in terms of drug delivery and the bio-availability factor of these drugs is known to be very high. Nanoparticles show a considerably good therapeutic effect, act as better imaging agents, and results in improved diagnostic testing. Therefore, nanoparticles have a huge positive impact on pharmaceuticals and healthcare units.

Nanotechnology

Nanotechnology is a broader term and it is holistically defined as ‘ The design, characterization, production, and application of the structures, devices, and systems by controlled manipulation of size and shape at the nanometer scale, that produces structures, devices or systems with at least one novel characteristics or property.

What is Nanomedicine?

Nanomedicine is the application of Nanotechnology to medicine. Nanomedicine employs nanoparticles to enhance the action of drugs in various processes. Generally, Nanoparticles act as a medium of transport for drugs that can reach areas where normal drugs wouldn’t be able to go on their own.

Mechanism of Nanoparticles

The nanoparticle drug-delivery systems can work in different ways. It carries the drug for delivery and can also be engineered to carry specific compounds that will let them bind, or attach, to molecules on tumor cells. Once attached, they can safely deliver the drug to the specific tumor site. Nanoparticles can also help with drug solubility. For a drug to work, it must be able to enter the bloodstream, which means it needs to be soluble.

Tumors commonly have disordered and leaky blood vessels sprouting through and off them. These vessels allow chemotherapy drugs to readily enter the tumor, but because chemotherapy molecules are so small, they also diffuse through the vessels and leak out of the tumor, attacking surrounding tissues. Nanoparticles are larger molecules that get trapped inside the tumor, where they do all the damage. Once they have delivered their drug cargo to cells, these nanoparticles can be designed to break down into harmless byproducts. (Click here for Reference)

However the efficacy of drug delivery through nanomedicine is largely based upon: a) efficient encapsulation of the drugs, b) successful delivery of drugs to the targeted region of the body, and c) successful release of the drugs.

Types of Nanoparticles

• Dendrimers: Long circulatory agents, used in controlled delivery of bioactives, targeted delivery of bioactives to macrophages, liver targeting etc.
• Liposomes: Phospholipid vesicles, biocompatible, versatile with good entrapment efficiency. It offers passive and active delivery of gene, protein, peptide and various other biomolecules. These liposomes also help to increase the functionality and decrease the damage that the drug does to the heart muscles specifically.
• Metallic Nanoparticles: Gold and silver colloids, with very small size resulting in high surface area available for functionalization. Used in drug and gene delivery, highly sensitive diagnostic assays, thermal ablation and radiotherapy enhancement.
• Nanocrystals Quantum dots: Provides bright fluorescence, narrow emission, Broad UV excitation and high photo stability. Long term multiple color imaging of liver cell; DNA hybridization, immunoassay.
• Polymeric micelles: Allows high drug entrapment, payload, biostability. Long circulatory, target specific active and passive drug delivery, diagnostic value.
• Polymeric nanoparticles: It is Biodegradable, biocompatible, offers complete drug protection. Excellent carrier for controlled and sustained delivery of drugs. Stealth and surface modified nanoparticles can be used for active and passive delivery of bioactives.
• DNA origami: DNA structures folded at nano level, which could have applications in drug delivery and even Nano robotics that can act as biological computers.

Need for Nanomedicine

• Target specific drug delivery results in more rapid onset of Drug action.
• Targeted drug delivery by Nanoparticles eliminates the possibility of side effects and reduces consequent cost of medications.
• Nanomedicine aims on maximising the bioavailability factor both at the targeted place and over the stipulated time period.
• Since the size of nanoparticle is much smaller when compared to other drug molecules, it has increased surface area.
• Nanoparticles are under research for their potential to decrease antibiotic resistance for various antimicrobial uses.
• Nanoparticles might also be used to circumvent multidrug resistance (MDR) mechanisms.
• A benefit of using nanoscale for medical technologies is that smaller devices are less invasive and can possibly be implanted inside the body.
• Biochemical reaction times are much shorter for nanoscale devices. These devices are faster and more sensitive than typical drug delivery.

Applications of Nanoparticles

Cancer Therapy:

The most practiced therapy for cancer treatment is chemotherapy, although it has the potential to cure cancer to a major extent, the damage caused to the other body tissues leaves the patient to cope up with many side effects. Nanoparticles have come up to rescue with excellent drug delivery systems. The nanoparticles used in cancer therapy are mostly micellar in nature. Micelles are also a great way to make insoluble drugs soluble due to their hydrophobic core and a hydrophilic shell. If the micelle’s surface is further PEGylated, it increases the ability of the nanocarriers to get through fenestrated capillaries of tumors and inflamed tissue through passive transport, thus resulting in higher drug concentration in tumors (Syed A.A. Rizvi and Ayman M. Saleh, et. Al. 2017).

Abraxane (albumin-bound paclitaxel) was approved by the U.S. Food and Drug Administration (FDA) to treat breast cancer and pancreatic cancer. The nanoparticle Onivyde, liposome-encapsulated irinotecan to treat metastatic pancreatic cancer, was approved by FDA in October 2015

Diagnostic testing

Current technology for diagnostic testing is hindered by the inadequacies of fluorescent markers including fading of fluorescence after a single use, color matching, and restricted use of dyes due to a bleeding effect, fluorescent nanoparticles provide researchers with the answer to overcome these disadvantages. Recently, theranostic nanoparticles, nanoparticles that can be used for treatment as well as diagnoses have gained much attention. This strategy has been realized in many classes of nanoparticles including, drug conjugates, dendrimers, surfactant aggregates (micelles and vesicles), core-shell particles, and carbon nanotubes. By combing both drug and imaging agents in one smart formulation, it is possible to monitor the pathway and localization of these nanoparticles at the target site as well as drug action to assess therapeutic response.

HIV/AIDS Treatment

Initially the treatment involved taking 30-40 pills per day. In the past decade, there have been advancements in therapeutics to reduce the pill count down to just a few each day. Research has shown a way to make this therapy even more effective by creating polymeric nanoparticles that deliver antiretroviral (ARV) drugs intracellularly as well as to the brain. This technology can also be used in adjunct with vaccinations to prevent HIV infections. The investigators used poly(lactic-co-glycolic acid) (PLGA) to prepare nanoparticles entrapping three antiretroviral drugs, ritonavir, lopinavir, and efavirenz. This nanoparticle system yielded sustained drug release for over 4 weeks (28 days), while free drugs were eliminated within 48 h (2 days). Nanoparticles are also known to be able to cross BBB by endocytosis/phagocytosis and many reports exist showing successful delivery of anti-HIV medications.

Doxil was originally approved by the FDA for the use on HIV-related Kaposi’s sarcoma. It is now being used to also treat ovarian cancer and multiple myeloma. The drug is encased in liposomes, which helps to extend the life of the drug that is being distributed. Doxil is the first nanomedicine to be approved by the US FDA in 1995.

Nutraceuticals

Nutraceuticals are food derived, standardized components with noticeable health benefits. Most nutraceuticals are lipophilic molecules, such as fat-soluble vitamins (A, D, E and K), polyunsaturated lipids and other phytochemicals. Nanotechnology again offers comprehensive assistance and most of the investigations have been aimed at improving the dissolution mechanisms of nutraceuticals via nanoparticle formulations. colloidal nanoparticles of curcumin dubbed, Theracurmin when compared to curcumin powder, exhibited 40-fold higher area under the curve (AUC) in rats and 27-fold higher in healthy human volunteers as well as inhibitory actions against alcohol intoxication.

Safety Issues of Nanoparticles

Along with the success of nanoparticles as nanomedicine, it is also important to evaluate the safety measures of nanomedicines in order to achieve biocompatibility and avoid any sort of damage in the long run. Many of the nanotherapeutics that are currently used in the clinic, such as Abraxane and Doxil, actually serve to reduce the toxicity of the encapsulated drugs. However, a small subset of nanoparticles that are currently undergoing preclinical investigation, e.g. carbon and metal-based nanoparticles, typically display cytotoxic properties. Nevertheless, the inherent toxic properties of such nanoparticles could be exploited to ablate diseased tissue, as long as healthy organs are protected through selective targeting. Moreover, there are several strategies (e.g. surface modification) that can be utilized to eliminate toxicity.

Conclusion and Future Scope

Nanomedicine is revolutionising the current approach towards disease treatment, diagnosis and various other branches of medical sciences. The unique properties of Nanoparticles makes it an excellent agent to be employed in pharmaceuticals and healthcare sectors. Through the manipulation of molecular size and surface properties, researchers are able to deliver drugs for a longer period of time with less frequent dosing (sustained-release) and with greater precision and penetration in difficult to access tissues. The possible cytotoxic properties of certain nanoparticles should be taken care by surface modification, pretreatment with immunomodulators  etc. Moreover, The use of Nanomedicine along with Artificial Intelligence will open doors for more customizable drugs with safer treatment options.