Doxorubicin (Dox) is the most widely used chemotherapeutic agent and is considered a highly powerful and broad-spectrum for cancer treatment. However, its application is compromised by the cumulative side effect of dose-dependent cardiotoxicity. Because of this, targeted drug delivery systems (DDS) are currently being explored in an attempt to reduce Dox systemic side-effects. In this study, DDS targeting hepatocellular carcinoma (HCC) has been designed, specifically to the asialoglycoprotein receptor (ASGPR). Dox-loaded albumin-albumin/lactosylated (core-shell) nanoparticles (tBSA/BSALac NPs) with low (LC) and high (HC) crosslink using glutaraldehyde were synthesized. Nanoparticles presented spherical shapes with a size distribution of 257 ± 14 nm and 254 ± 14 nm, as well as an estimated surface charge of −28.0 ± 0.1 mV and −26.0 ± 0.2 mV, respectively. The encapsulation efficiency of Dox for the two types of nanoparticles was higher than 80%. The in vitro drug release results showed a sustained and controlled release profile. Additionally, the nanoparticles were revealed to be biocompatible with red blood cells (RBCs) and human liver cancer cells (HepG2 cells). In cytotoxicity assays, Dox-loaded nanoparticles decrease cell viability more efficiently than free Dox. Specific biorecognition assays confirmed the interaction between nanoparticles and HepG2 cells, especially with ASGPRs. Both types of nanoparticles may be possible DDS specifically targeting HCC, thus reducing side effects, mainly cardiotoxicity. Therefore, improving the quality of life from patients during chemotherapy.

Hepatocellular carcinoma (HCC) ranks fifth in occurrence and second in mortality of all cancers. The development of effective therapies for HCC is urgently needed. Anticancer drugs targeted to the liver-specific asialoglycoprotein receptors (ASGPRs) are viewed as a promising potential treatment for HCC. ASGPRs facilitate the recognition and endocytosis of molecules, and possibly vehicles with galactose end groups, by the liver. In this study, bovine serum albumin (BSA) was conjugated with lactose using a thermal treatment. The formation of lactosylated BSA (BSA-Lac) was confirmed by a change of the chemical structure, increased molecular mass, and Ricinus communis lectin recognition. Subsequently, the low-crosslinking BSA-Lac nanoparticles (LC BSA-Lac NPs) and high-crosslinking BSA-Lac nanoparticles (HC BSA-Lac NPs) were synthesized. These nanoparticles presented spherical shapes with a size distribution of 560 ± 18.0 nm and 539 ± 9.0 nm, as well as an estimated surface charge of −26 ± 0.15 mV and −24 ± 0.45 mV, respectively. Both BSA-Lac NPs were selectively recognized by ASGPRs as shown by biorecognition, competition, and inhibition assays using an in vitro model of HCC. This justifies pursuing the strategy of using BSA-Lac NPs as potential drug nanovehicles with selective direction toward hepatocellular carcinoma.

In this work, we report the evaluation of lactosylated graphene oxide (GO-AL) as a potential drug carrier targeted at an asialoglycoprotein receptor (ASGPR) from hepatic cancer cells. Structural-modification, safety evaluation, and functional analysis of GO-AL were performed. The structure and morphology of the composite were analyzed by scanning electron microscopy (SEM) and atomic force microscopy (AFM), while Raman and FTIR spectroscopy were used to track the chemical modification. For the safe application of GO-AL, an evaluation of the cytotoxic effect, hemolytic properties, and specific interactions of the glycoconjugate were also studied. SEM and AFM analysis of the GO showed graphene sheets with a layer size of 2–3 nm, though a few of them reached 4 nm. The Raman spectra presented characteristic peaks of graphene oxide at 1608 cm⁻¹ and 1350 cm⁻¹, corresponding to G and D bands, respectively. Besides, Si–O peaks for the APTES conjugates of GO were identified by FTIR spectroscopy. No cytotoxic or hemolytic effects were observed for GO samples, thus proving their biocompatibility. The interaction of Ricinus communis lectin confirmed that GO-AL has a biorecognition capability and an exposed galactose structure. This biorecognition capability was accompanied by the determination of the specific absorption of lactosylated GO by HepG2 cells mediated through the asialoglycoprotein receptor. The successful conjugation, hemolytic safety, and specific recognition described here for lactosylated GO indicate its promise as an efficient drug-delivery vehicle to hepatic tissue.

El cáncer de tiroides (CT) es una de las neoplasias endocrinas frecuentes con una incidencia en aumento a nivel mundial. Los tipos más comunes de CT incluyen el carcinoma papilar, folicular, oncocítico, medular y el agresivo carcinoma anaplásico. A pesar de los tratamientos como la cirugía y el yodo radiactivo, entre el 7 % y el 23 % de los pacientes pueden desarrollar metástasis resistentes a la terapia. El objetivo de esta revisión fue demostrar el potencial terapéutico de las nanopartículas (NP) aplicada en el CT. Se realizó una búsqueda bibliográfica en PubMed, Embase, Web of Science, Elsevier y Scielo, seleccionando un total de 41 artículos conforme a los lineamientos de la escala para la evaluación de artículos de revisión narrativa (SANRA). Las palabras clave se definieron mediante el uso de la guía Medical Subject Heading (MeSH). Los resultados evidencian que las NP mejoran la biodisponibilidad de los fármacos, reducen efectos adversos y permiten una liberación controlada de agentes terapéuticos. Formulaciones como nanoemulsiones, liposomas, NP híbridas y fototérmicas demuestran un alto potencial en la focalización tumoral. En conjunto, las NP representan un enfoque prometedor y altamente específico para optimizar el tratamiento del CT y superar las limitaciones de las terapias tradicionales.