Graphene oxide nanoribbons conjugated with 1, 2-distearoyl-sn-glycero-3 phosphoethanolamine-poly (ethylene glycol)-transferrin enhanced targeted delivery and cytotoxicity of raloxifene against breast cancer.

The clinical utility of raloxifene (RLX), a selective estrogen receptor modulator (SERM), has been compromised by severe side effects and unfavorable drug properties. To address these, a transferrin (Tf) conjugated graphene oxide nanoribbon (GONR) platform was tried for RLX. The stability of GONRs in biological media was improved by surface modification with 1, 2-Distearoyl-sn-glycero-3 phosphoethanolamine-Poly (ethylene glycol) (DSPE-PEG). The Tf molecule was covalently attached to DSPE-PEG (DPT) using EDC-NHS chemistry. The surface of GONR was then modified with DSPE-PEG (DP) or DPT and loaded with RLX (GDP-RLX and GDPT-RLX). The final formulations were characterized for drug loading and stability. The anticancer activities of pure RLX, GDP-RLX, and GDPT-RLX were evaluated and compared in all the in vitro and in vivo studies. In vitro cell line studies showed that GDPT-RLX have significantly high cytotoxicity, cellular uptake, apoptosis induction, G2/M phase arrest, anti-migration properties, and apoptotic protein expression, followed by GDP-RLX and RLX. Pharmacokinetics and tumor biodistribution were also found to be excellent with GDPT-RLX. The in vivo tumor therapy and tumor evaluation outcomes were also consistent with the in vitro data. The Tf conjugated GDPT-RLX represents a promising approach for targeted and sustained delivery of RLX with enhanced therapeutic efficacy.

An Update on Emergent Nano-Therapeutic Strategies against Pediatric Brain Tumors.

Pediatric brain tumors are the major cause of pediatric cancer mortality. They comprise a diverse group of tumors with different developmental origins, genetic profiles, therapeutic options, and outcomes. Despite many technological advancements, the treatment of pediatric brain cancers has remained a challenge. Treatment options for pediatric brain cancers have been ineffective due to non-specificity, inability to cross the blood-brain barrier, and causing off-target side effects. In recent years, nanotechnological advancements in the medical field have proven to be effective in curing challenging cancers like brain tumors. Moreover, nanoparticles have emerged successfully, particularly in carrying larger payloads, as well as their stability, safety, and efficacy monitoring. In the present review, we will emphasize pediatric brain cancers, barriers to treating these cancers, and novel treatment options.

Oral insulin delivery: Barriers, strategies, and formulation approaches: A comprehensive review.

Diabetes Mellitus is characterized by a hyperglycemic condition which can either be caused by the destruction of the beta cells or by the resistance developed against insulin in the cells. Insulin is a peptide hormone that regulates the metabolism of carbohydrates, proteins, and fats. Type 1 Diabetes Mellitus needs the use of Insulin for efficient management. However invasive methods of administration may lead to reduced adherence by the patients. Hence there is a need for a non-invasive method of administration. Oral Insulin has several merits over the conventional method including patient compliance, and reduced cost, and it also mimics endogenous insulin and hence reaches the liver by the portal vein at a higher concentration and thereby showing improved efficiency. However oral Insulin must pass through several barriers in the gastrointestinal tract. Some strategies that could be utilized to bypass these barriers include the use of permeation enhancers, absorption enhancers, use of suitable polymers, use of suitable carriers, and other agents. Several formulation types have been explored for the oral delivery of Insulin like hydrogels, capsules, tablets, and patches which have been described briefly by the article. A lot of attempts have been made for developing oral insulin delivery however none of them have been commercialized due to numerous shortcomings. Currently, there are several formulations from the companies that are still in the clinical phase, the success or failure of some is yet to be seen in the future.

Bioinspired and biomimetic micro- and nanostructures in biomedicine.

Bioinspired and biomimetic micro- and nanostructures have a high significance in the field of biomedicine. In this review, the possible applications of these micro- and nanostructures that come across in our daily life and inspired by nature itself are presented. Also, the biomimetic and bioinspired systems related to micro- and nanostructures in biomedicine are also described. The role of bioinspired and biomimetic micro- and nanostructures in therapeutics, especially in anti-inflammatory and wound healing, development of bioinspired medical devices, tissue engineering, drug delivery, gene delivery, pressure sensors, and bioprinting are discussed. The biomimetic and bioinspired systems using carbon-based nanostructures, polymer nanocomposites, hybrid scaffolds, polymer networks,and protein nanostructures are also reviewed. The advantage of these bioinspired and biomimetic structures is derived from their high biocompatibility when compared to the synthetically derived micro-/nanostructures. By developing deeper knowledge and overcoming the associated challenges, these micro- and nanostructures present a promising solution for many unresolved problems in biomedicine.

Strategies to Improve Insulin Delivery through Oral Route: A Review.

Diabetes mellitus is found to be among the most suffered and lethal diseases for mankind. Diabetes mellitus type-1 is caused by the demolition of pancreatic islets responsible for the secretion of insulin. Insulin is the peptide hormone (anabolic) that regulates the metabolism of carbohydrates, fats, and proteins. Upon the breakdown of the natural process of metabolism, the condition leads to hyperglycemia (increased blood glucose levels). Hyperglycemia demands outsourcing of insulin. The subcutaneous route was found to be the most stable route of insulin administration but faces patient compliance problems. Oral Insulin delivery systems are the patient-centered and innovative novel drug delivery system, eliminating the pain caused by the subcutaneous route of administration. Insulin comes in contact across various barriers in the gastrointestinal tract, which has been discussed in detail in this review. The review describes about the different bioengineered formulations, including microcarriers, nanocarriers, Self-Microemulsifying Drug Delivery Systems (SMEDDs), Self-Nanoemulsifying drug delivery systems (SNEDDs), polymeric micelles, cochleates, etc. Surface modification of the carriers is also possible by developing ligand anchored bioconjugates. A study on evaluation has shown that the carrier systems facilitate drug encapsulation without tampering the properties of insulin. Carrier-mediated transport by the use of natural, semi-synthetic, and synthetic polymers have shown efficient results in drug delivery by protecting insulin from harmful environment. This makes the formulation readily acceptable for a variety of populations. The present review focuses on the properties, barriers present in the GI tract, overcome the barriers, strategies to formulate oral insulin formulation by enhancing the stability and bioavailability of insulin.

Carbon Nanotubes: Current Perspectives on Diverse Applications in Targeted Drug Delivery and Therapies.

Current discoveries as well as research findings on various types of carbon nanostructures have inspired research into their utilization in a number of fields. These carbon nanostructures offer uses in pharmacy, medicine and different therapies. One such unique carbon nanostructure includes carbon nanotubes (CNTs), which are one-dimensional allotropes of carbon nanostructure that can have a length-to-diameter ratio greater than 1,000,000. After their discovery, CNTs have drawn extensive research attention due to their excellent material properties. Their physical, chemical and electronic properties are excellent and their composites provide great possibilities for enormous nanometer applications. The current study provides a systematic review based on prior literature review and data gathered from various sources. The various research studies from many research labs and organizations were systematically retrieved, collected, compiled and written. The entire collection and compilation of this review concluded the use of CNT approaches and their efficacy and safety for the treatment of various diseases such as brain tumors or cancer via nanotechnology-based drug delivery, phototherapy, gene therapy, antiviral therapy, antifungal therapy, antibacterial therapy and other biomedical applications. The current review covers diverse applications of CNTs in designing a range of targeted drug delivery systems and application for various therapies. It concludes with a discussion on how CNTs based medicines can expand in the future.

Graphene nanoribbon: An emerging and efficient flat molecular platform for advanced biosensing.

Graphene nanoribbons (GNRs) are lengthened one-dimensional monolayer strips of graphene and have a hexagonal honeycomb lattice structure. The captivating properties like electrical conductivity, emerging band gap, optical property, thermal conductivity, high mechanical strength, and ultrahigh surface area make them a better candidate for biomedical applications. The properties can be significantly reformed and controlled by altering the edge functionalities and geometry. The exhibition of a wide potential window coupled with an ultra-high surface area to host sensing element makes GNR an excellent biosensing platform. Consequently, biosensing is one of the most explored applications of GNR. This review presents an overview of the characteristics, methods of synthesis, and biosensing applications of GNR. Overall, GNR is considered a promising platform for efficient signal transduction compared to conventional biosensing platforms. Further, it offers high electrical conductivity, large surface area, high adsorption, synergistic effects with combined materials, fast response, sensitivity, and selectivity.

Advanced drug delivery applications of layered double hydroxide.

Layered double hydroxides (LDHs), also known as anionic clays or hydrotalcite-like compounds, are a class of nanomaterials that attained great attention as a carrier for drug delivery applications. The lamellar structure of this compound exhibits a high surface-to-volume ratio which enables the intercalation of therapeutic agents and releases them at the target site, thereby reducing the adverse effect. Moreover, the intercalated drug can be released in a sustained manner, and hence the frequency of drug administration can be decreased. The co-precipitation, ion exchange, manual grinding, and sol-gel methods are the most employed for their synthesis. The unique properties like the ease of synthesis, low cost, high biocompatibility, and low toxicity render them suitable for biomedical applications. This review presents the advances in the structure, properties, method of preparation, types, functionalization, and drug delivery applications of LDH. Also, this review provides various new conceptual insights that can form the basis for new research questions related to the drug delivery applications of LDH.

Graphene nanoribbons: A promising nanomaterial for biomedical applications.

Graphene nanoribbons (GNRs) are narrow lengthened strips of single-layer graphene. Among the graphene family of nanomaterials, GNRs are remarkable materials due to their attractive physical, chemical, electrical, mechanical, thermal, and optical properties. They have an ultra-high surface area. Graphene-oxide nanoribbons (GONRs), the oxygenated derivative of GNRs, offer more possibilities in the biomedicine due to their amphiphilic nature. Noncovalent and covalent modifications of these are possible for advanced biomedical applications. This review describes the properties, synthesis, surface modifications, and toxicities of GNRs, along with their biomedical applications. Their applications in drug delivery, anticancer therapy, sensing, antimicrobial therapy, imaging, gene therapy, photothermal therapy, management of spinal cord injury, bone regeneration, etc. are reviewed.