Nanotechnology: an effective tool for enhancing bioavailability and bioactivity of phytomedicine
To achieve the desired therapeutic objective, the drug product must deliver the active drug at an optimal rate and amount. By proper biopharmaceutic design, the rate and extent of drug absorption (also called as bioavailability) or the systemic delivery of drugs to the body can be varied from rapid and complete absorption to slow and sustained absorption depending upon the desired therapeutic objective. Phytomedicine have served as the foundation for a larger fraction of the current pharmacopeia. But the delivery of phytomedicine is always problematic due to poor aqueous solubility, poor permeation, low systemic availability, instability and extensive first pass metabolism. Current review will discuss in detail about how nanotechnology can enhance the bioavilability and bioactivity of the phytomedicine.
Gunasekaran T, Haile T, Nigusse T, Dhanaraju MD. Nanotechnology: an effective tool for enhancing bioavailability and bioactivity of phytomedicine. Asian Pac J Trop Biomed. 2014;4(Suppl 1):S1–S7.
Nanoemulsion-based delivery system for enhanced oral bioavailability and caco-2 cell monolayers permeability of berberine hydrochloride.
Berberine hydrochloride (BBH) has a variety of pharmacological activities such as antitumor, antimicrobial, anti-inflammation, and reduce irritable bowel syndrome. However, poor stability and low oral bioavailability limited its usage. Herein, an oil-in-water nanoemulsion system of BBH was developed to improve its stability and oral bioavailability. The pseudoternary phase diagrams were constructed for the determination of composition of various nanoemulsions. The nanoemulsions of BBH composed of Labrafil M 1944 CS (oil phase), RH-40 (surfactant), glycerin (co-surfactant), and water (aqueous phase). The O/W nanoemulsion of BBH showed a relative bioavailability of 440.40% compared with unencapsulated BBH and was stable in our 6-month stability study. Further, there was a significant increase in intestinal permeability of BBH as assessed by Caco-2 cell monolayers and a significant reduction in efflux of BBH by the multidrug efflux pump P-glycoprotein. This study confirmed that the nanoemulsion formulation could be used as an alternative oral formulation of BBH to improve its stability, oral bioavailability and permeability.
Yong-Jiang Li, Xiong-Bin Hu, Xiu-Ling Lu, De-Hua Liao, Tian-Tian Tang, Jun-Yong Wu & Da-Xiong Xiang (2017) Nanoemulsion-based delivery system for enhanced oral bioavailability and Caco-2 cell monolayers permeability of berberine hydrochloride, Drug Delivery, 24:1, 1868-1873
Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide
Andrographolide (AG), a compound with low water solubility, possesses various pharmacological activities, particularly anti-inflammatory activity. However, its low oral bioavailability is a major obstacle to its potential use. This study developed and optimized an AG-loaded nanoemulsion (AG-NE) formulation to improve AG oral bioavailability and its protective effects against inflammatory bowel disease.
A high-pressure homogenization technique was used to prepare the AG-NE and solubility, viscosity, and droplet size tests were conducted to develop the optimized AG-NE composed of α-tocopherol, ethanol, Cremophor EL, and water. The permeability was assessed using everted rat gut sac method and in vivo absorption and anti-inflammatory effect in rats was also evaluated. The plasma concentration of AG was determined using our validated high performance liquid chromatography method, which was used to generate a linear calibration curve over the concentration range of 0.1–25 μg/mL in rat plasma (R2>0.999).
The optimized AG-NE had a droplet size of 122±11 nm confirmed using transmission electron microscopy and a viscosity of 28 centipoise (cps). It was stable at 4 and 25°C for 90 days. An ex vitro intestinal permeability study indicated that the jejunum was the optimal site for AG absorption from the optimized AG-NE, which was 8.21 and 1.40 times higher than that from an AG suspension and AG ethanol solution, respectively. The pharmacokinetic results indicate that the absorption of AG from AG-NE was significantly enhanced in comparison with that from the AG suspension, with a relative bioavailability of 594.3%. Moreover, the ulcer index and histological damage score of mice with indomethacin-induced intestinal lesions were significantly reduced by AG-NE pretreatment.
We conclude that the developed AG-NE not only enhanced the oral bioavailability of AG in this study but may also prove to be an effective formulation of AG for preventing gastrointestinal inflammatory disorders.
Yen CC, Chen YC, Wu MT, Wang CC, Wu YT. Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide. Int J Nanomedicine. 2018;13:669–680. Published 2018 Jan 31.
Bioavailability and Delivery of Nutraceuticals Using Nanotechnology
ABSTRACT: Nanotechnology is an enable technology that has the potential to revolutionize agriculture and food systems. Driven by increasing consumer demand for healthy food products, researchers have been applying tools and knowledge in nanotechnology to address the issues relevant to food and nutrition. This concise review is mainly focused on nanoemulsions and polymer micelles‐based delivery systems which have shown enhanced oral bioavailability and biological efficacies (that is, antiinflammation, anti‐cancer, and so on) of different phytochemicals. Nanoemulsions are a class of extremely small droplets that appear to be transparent or translucent with a bluish coloration. They are usually in the range 50 to 200 nm but much smaller than the range (from 1 to 100 μm) for conventional emulsions. Nanoemulsion preparation, characterization, and bioavailability have been discussed. Curcumin nanoemulsions show 85% inhibition of TPA‐induced mouse ear inflammation as well as the inhibition of cyclin D1 expression, while dibenzoylmethane (DBM) nanoemulsion shows about 3‐fold increase in oral bioavailability compared to the conventional DBM emulsion. Biopolymer micelles show significantly improved water solubility/dispersibility and in vitro anti‐cancer activity of phytochemicals. More research efforts are still needed for the understanding of the potential impacts of nanoencapsulated phytochemicals on the human body and environment to address the public concerns.
Role of Nanotechnology in Cosmeceuticals: A Review of Recent Advances
Nanotechnology manifests the progression in the arena of research and development, by increasing the efficacy of the product through delivery of innovative solutions. To overcome certain drawbacks associated with the traditional products, application of nanotechnology is escalating in the area of cosmeceuticals. Cosmeceuticals are regarded as the fastest growing segment of the personal care industry and the use has risen drastically over the years. Nanocosmeceuticals used for skin, hair, nail, and lip care, for conditions like wrinkles, photoaging, hyperpigmentation, dandruff, and hair damage, have come into widespread use. Novel nanocarriers like liposomes, niosomes, nanoemulsions, microemulsion, solid lipid nanoparticles, nanostructured lipid carrier, and nanospheres have replaced the usage of conventional delivery system. These novel nanocarriers have advantages of enhanced skin penetration, controlled and sustained drug release, higher stability, site specific targeting, and high entrapment efficiency. However, nanotoxicological researches have indicated concern regarding the impact of increased use of nanoparticles in cosmeceuticals as there are possibilities of nanoparticles to penetrate through skin and cause health hazards. This review on nanotechnology used in cosmeceuticals highlights the various novel carriers used for the delivery of cosmeceuticals, their positive and negative aspects, marketed formulations, toxicity, and regulations of nanocosmeceuticals.
Shreya Kaul, Neha Gulati, Deepali Verma, Siddhartha Mukherjee, and Upendra Nagaich, “Role of Nanotechnology in Cosmeceuticals: A Review of Recent Advances,” Journal of Pharmaceutics, vol. 2018, Article ID 3420204, 19 pages, 2018.