Mechanistic analysis of solute transport in an in vitro physiological two‐phase dissolution apparatus

Solid lipid nanoparticles and nanostructured lipid carriers: A review emphasizing on particle structure and drug release

There has been a surge of interest in the development of nanoscale systems for the encapsulation, protection, and delivery of lipophilic nutrients, vitamins, and nutraceuticals. This review article highlights the challenges associated with incorporating these lipophilic bioactive components into foods, and then discusses potential nanoscale delivery systems that can be used to overcome these challenges. In particular, the desirable characteristics required for any nanoscale delivery system are presented, as well as methods of fabricating them and of characterizing them. An overview of different delivery systems is given, such as microemulsions, nanoemulsions, emulsions, microgels, and biopolymer nanoparticles, and their potential applications are discussed. Nanoscale delivery systems have considerable potential within the food industry, but they must be carefully formulated to ensure that they are safe, economically viable, and effective.

Nanoscale Nutrient Delivery Systems for Food Applications: Improving Bioactive Dispersibility, Stability, and Bioavailability

The transdermal route of drugs has received increased attention in recent years due to numerous advantages over the oral and injectable routes, such as avoidance of the hepatic metabolism, protection of drugs from the gastrointestinal tract, sustained drug delivery, and good patient compliance. The assessment of ex vivo permeation during the pharmaceutical development process helps in understanding the product quality and performance of a transdermal delivery system. Generally, excised human skin relevant to the application site or animal skin is recommended for ex vivo permeation studies. However, the limited availability of the human skin and ethical issues surrounding the use of animal skin rendered these models less attractive in the permeation study. In the last three decades, enormous efforts have been put into developing artificial membranes and 3D cultured human skin models as surrogates to the human skin. This manuscript provides an insight on the European Medicines Agency (EMA) guidelines for permeation studies and the parameters affected when using Franz diffusion cells in the permeation study. The need and possibilities for skin alternatives, such as artificially cultured human skin models, parallel artificial membrane permeability assays (PAMPA), and artificial membranes for penetration and permeation studies, are comprehensively discussed.

Alternatives to Biological Skin in Permeation Studies: Current Trends and Possibilities.

Recent advances in the design of food matrices to improve the bioavailability of bioactive food components, such as nutraceuticals and vitamins, are reviewed. Nutraceuticals may be isolated from their natural origin and then incorporated into functional food products as functional ingredients. In this case, specially designed colloidal delivery systems are often needed to improve their dispersibility, stability, food compatibility, and bioavailability. Alternatively, nutraceuticals may be delivered as part of natural foods, such as fruits and vegetables. In this case, their bioavailability can be improved by consuming them with food matrices specifically designed to increase their bioavailability, that is, excipient foods. The utility of a new scheme (NuBACS) for classifying the major factors limiting the oral bioavailability of nutraceuticals is also highlighted.

Enhancing nutraceutical bioavailability through food matrix design

Since their introduction in the early 1990s, solid lipid nanoparticles (SLNs) have received tremendous attention in drug delivery because of their ability to carry and solubilize lipophilic drugs and their small particle size, resulting in increased cellular uptake and absorption. SLNs are composed of physiological lipids, which reduce the risk of acute and chronic toxicity. However, SLNs are prone to instabilities because of their complex crystallization behavior due to the occurrence of polymorphic transitions. This chapter summarizes various aspects of SLNs such as components and production of SLNs, drug loading, drug release, stability, and application of SLNs in drug delivery. This chapter also provides a summary of SLNs as a potential carrier of anticancer drugs, one of the most aggressively expanding areas of research. A special emphasis is placed on the stability and toxicity issues associated with SLNs and their diagnostic applications.

Solid Lipid Nanoparticles in Drug Delivery: Opportunities and Challenges

Low frequency ultrasound-assisted drug delivery has been widely investigated as a non-invasive method to enhance the transdermal penetration of drugs. Using this technique, a brief application of ultrasound is used to permeabilize skin for a prolonged time. In this review, an overview on ultrasound is detailed to help explain the parameters that could be modulated to obtain the desired ultrasound parameters for enhanced transdermal drug delivery. The mechanisms of enhancement and the latest developments in the area of ultrasound-assisted transdermal drug delivery are discussed. Special emphasis is placed on the effects of ultrasound when used in combination with microneedles, electroporation and iontophoresis, and penetration enhancers. Further, this review summarizes the effect of ultrasound on skin integrity and the regulatory requirements for commercialization of the ultrasound based transdermal delivery instruments.

Advances in Ultrasound Mediated Transdermal Drug Delivery.

Elucidation of the orientation of selected drugs with 2-hydroxylpropyl-β-cyclodextrin using 2D-NMR spectroscopy and molecular modeling.

Diabetes is a prime risk factor in cardiovascular disease (CVD), which includes peripheral vascular disease, coronary artery disease, and cerebrovascular disease. Management of cardiovascular dysfunctions associated with diabetes has been a challenge for decades. The nutraceutical approach for prevention of diabetic cardiovascular complications has been a considerably newer trend. Nutraceuticals are medicinal foods that help in maintaining the health of individuals, thereby preventing or treating diseases. A literature search showed that several nutraceuticals used as dietary supplements have the ability to reduce cardiovascular risk factors. Thus, the nutraceutical approach can be very promising in the treatment of diabetic cardiovascular complications. In this review, we summarize the recent research findings on dietary fiber, antioxidants, prebiotics, and probiotics to highlight the benefits of using nutraceuticals in the management of diabetes-associated cardiovascular dysfunctions.

Nutraceutical Approaches in the Management of Cardiovascular Dysfunctions Associated with Diabetes Mellitus

The purpose of this work was to design and characterize a topical formulation of econazole nitrate (EN) with potential for treating Raynaud's phenomenon (RP). Four topical dosage forms (F1_topical solution, F2_HPMC or hydroxypropyl methylcellulose dispersion, F3_VersaBase® cream, and F4_Lipoderm® Activemax™ Cream) containing 3% w/w EN were prepared and characterized for drug content, pH, viscosity, spreadability, drug crystallinity, stability, and in vitro permeation using Franz cells across pig ear skin, and results were compared to the 1% marketed EN cream. All four formulations had acceptable physical and visual characteristics required for topical application, with 3% w/w EN. The order of amount of drug permeated from highest to lowest was F2 (10.27%) > F4 (2.47%) > F1 (2.28%) > F3 (1.47%) > marketed formulation (0.22%). Formulation F2 showed better penetration of the drug into the stratum corneum, epidermis, and dermis layers. The drug concentration in the stratum corneum and epidermis was approximately 10-20 times higher with F2 compared to the marketed formulation. All formulations were found to be stable for up to 6 months. All four EN formulations were found to be better than the 1% marketed cream. Formulation F2_HPMC dispersion could be further explored as a treatment option for RP.

Saloni Daftardar

Papers

Solid Lipid Nanoparticles in Drug Delivery: Opportunities and Challenges

Advances in Ultrasound Mediated Transdermal Drug Delivery.

Elucidation of the orientation of selected drugs with 2-hydroxylpropyl-β-cyclodextrin using 2D-NMR spectroscopy and molecular modeling.

Nutraceutical Approaches in the Management of Cardiovascular Dysfunctions Associated with Diabetes Mellitus

Evaluation of topical econazole nitrate formulations with potential for treating Raynaud’s phenomenon