Dendrimers based cancer nanotheranostics: An overview.

Cancer is a known deadliest disease that requires a judicious diagnostic, targeting, and treatment strategy for an early prognosis and selective therapy. The major pitfalls of the conventional approach are non-specificity in targeting, failure to precisely monitor therapy outcome, and cancer progression leading to malignancies. The unique physicochemical properties offered by nanotechnology derived nanocarriers have the potential to radically change the landscape of cancer diagnosis and therapeutic management. An integrative approach of utilizing both diagnostic and therapeutic functionality using a nanocarrier is termed as nanotheranostic. The nanotheranostics platform is designed in such a way that overcomes various biological barriers, efficiently targets the payload to the desired locus, and simultaneously supports planning, monitoring, and verification of treatment delivery to demonstrate an enhanced therapeutic efficacy. Thus, a nanotheranostic platform could potentially assist in drug targeting, image-guided focal therapy, drug release and distribution monitoring, predictionof treatment response, and patient stratification. A class of highly branched nanocarriers known as dendrimers is recognized as an advanced nanotheranostic platform that has the potential to revolutionize the oncology arena by its unique and exciting features. A dendrimer is a well-defined three-dimensional globular chemical architecture with a high level of monodispersity, amenability of precise size control, and surface functionalization. All the dendrimer properties exhibit a reproducible pharmacokinetic behavior that could ensure the desired biodistribution and efficacy. Dendrimers are thus being exploited as a nanotheranostic platform embodying a diverse class of therapeutic, imaging, and targeting moieties for cancer diagnosis and treatment.

The Gradually Expanding Scope for Biowaivers of Oral Products: An Overview.

The regulatory paradigm is relaxing gradually without compromising the safety, efficacy and the quality of the drug product and, most importantly, a perceptible scientific consensus is maturing towards the need of affordable medicines. The establishment of bioequivalence (BE) is no longer being considered to be accomplished only by in vivo studies in oral drug products. The potential use of in vitro dissolution testing in lieu of BE studies has now been regulatory adopted and is commonly referred to as "biowaiver". Further, the advent of biopharmaceutics classification system (BCS) and in vitro-in vivo correlation (IVIVC) proves to be sound milestones and signifies that we are incessantly forwarding towards a scenario that would reduce regulatory burden, save time and make the drug products more affordable while ensuring their quality. This review outlines, the current and pertinent regulatory environment for biowaiver based on in vitro drug dissolution, primarily as per the FDA perspective. The rationale used for qualification of biowaiver for different strengths, post-approval changes and multi-source products are discussed along with the role of BCS and IVIVC.

Self-emulsifying lipid formulation: an overview.

An important step in oral drug development is to identify drug candidates that show sufficient aqueous solubility and could resist or bypass first-pass metabolism in order to overcome bioavailability problems. Aqueous solubility is characteristically low for Biopharmaceutical Classification System (BCS) class II and class IV drug candidates. Several formulation approaches are being identified to overcome the low solubility aspect of a drug candidate such as particle size manipulation, solid dispersions, inclusion complexes and several of nanoparticle-based options. However, the formulation for drug candidates that in addition to low aqueous solubility shows high intestinal and first-pass metabolism is challenging. The self-emulsifying lipid formulations (SELF) provide a mean for sidestepping these factors and improve the bioavailability of lipophilic and highly first- pass metabolised drugs. Nevertheless, formulation of a successful SELF requires an exhaustive understanding of the component used to formulate them, the behaviour of the formulation within the gastrointestinal (GI) milieu and the mechanism by which the drug is released and absorbed. This review gives a brief description of the formulation aspects of SELF and their potential role to mitigate the bioavailability problem related to lipophilic and highly first- pass metabolised drugs.

Patents on brain permeable nanoparticles.

The blood-brain barrier (BBB) presents a combination of physical and electrostatic barriers. It is a highly complex structure that tightly regulates the movement of molecules from the blood to brain, protecting it from injuries and diseases. However, the BBB also significantly precludes the delivery of drugs to the brain, thus, preventing the therapy of a number of neurological disorders like brain cancer, epilepsy, Alzheimer's disease, schizophrenia etc. Numerous drug delivery strategies have been developed to circumvent this barrier. Out of those, one popular approach is the use of nanoparticles. Nanoparticles form solid, colloidal drug delivery system that consists of macromolecular materials in which the active principle is dissolved, entrapped or encapsulated or onto which the active principle is adsorbed or attached. Brain targeted polymeric nanoparticles have been found to increase the therapeutic efficacy and reduce the toxicity for a large number of drugs. By coating the nanoparticles with surfactants, higher concentrations of the drugs can be delivered. The article presents various approaches used in design and delivery of nanoparticles to brain. It also reviews various patents that describe the use of nanoparticles to deliver various neurotherapeutics to brain.

Brain permeable nanoparticles.

The brain is one of the least accessible organs of the body, thus making the delivery of neurotherapeutics almost a challenge. Despite its relatively high nutrient support and exchange requirements, the uptake of any compound is strictly regulated by the blood brain barrier (BBB). As a consequence, BBB prevents effective treatment of many severe and life threatening diseases like brain cancer, epilepsy, Alzheimer's disease, schizophrenia etc. Numerous drug delivery strategies have been developed to circumvent this barrier. One such approach is the use of nanoparticles. Nanoparticles form solid, colloidal drug delivery system that consists of macromolecular materials in which the active principle is dissolved, entrapped or encapsulated or onto which the active principle is adsorbed or attached. Brain targeted polymeric nanoparticles have been found to increase the therapeutic efficacy and reduce the toxicity for a large number of drugs. By coating the nanoparticles with surfactants, higher concentrations of drugs can be delivered to the brain. The article presents various approaches used in design and delivery of nanoparticles to brain. It also reviews various patents that describe the use of nanoparticles to deliver various neurotherapeutics and neurodiagnostics to brain.