Transferrin-modified liposomes triggered with ultrasound to treat HeLa cells

Abstract

Targeted liposomes are designed to target specific receptors overexpressed on the surfaces of cancer cells. This technique ensures site-specific drug delivery to reduce undesirable side effects while enhancing the efficiency of the encapsulated therapeutics. Upon reaching the tumor site, these liposomes can be triggered to release their content in a controlled manner using ultrasound (US). In this study, drug release from pegylated calcein-loaded liposomes modified with transferrin (Tf) and triggered with US was evaluated. Low-frequency ultrasound at 20-kHz using three different power densities (6.2 mW/cm2, 9 mW/cm2 and 10 mW/cm2) was found to increase calcein release. In addition, transferrin-conjugated pegylated liposomes (Tf-PEG liposomes) were found to be more sonosensitive compared to the non-targeted (control) liposomes. Calcein uptake by HeLa cells was found to be significantly higher with the Tf-PEG liposomes compared to the non-targeted control liposomes. This uptake was further enhanced following the exposure to low-frequency ultrasound (at 35 kHz). These findings show that targeted liposomes triggered with US have promising potential as a safe and effective drug delivery platform.

Development of Liposome-Based Immunoassay for the Detection of Cardiac Troponin I

“…In addition, dynamic light scattering (DLS) studies revealed the size range and % polydispersity (Pd) of the liposomes (Figure 1). The obtained Pd index value was found to be acceptable as it falls in the criteria of its upper limit of 20% for DLS measurements [51]. As shown in Table 1, even after 10 weeks of storage at 4 • C, the liposome solution was found to be stable, with minimal variation in their average radius (96.3 ± 3.9 nm), while maintaining a quenched load of calcein that was released upon the addition of Triton X-100, leading to a five-fold increase in the fluorescence signal.…”

“…The liposomes are a crucial component of the developed assay; hence, the preparation and characterization procedures of these nanocarriers are essential to ensure efficacy and reproducibility. Biotin-conjugated calcein-loaded liposomes were synthesized via the thin-film hydration method, similar to the previously reported studies [45,51], and a full characterization process was applied, including a Stewart assay, to quantify the total lipid concentration of the liposome solution, DSL measurements, and stability studies. The Stewart assay was conducted according to previously reported procedures [51], indicating a calculated total lipid concentration of 10.1 mmol/L.…”

“…Biotin-conjugated calcein-loaded liposomes were synthesized via the thin-film hydration method, similar to the previously reported studies [45,51], and a full characterization process was applied, including a Stewart assay, to quantify the total lipid concentration of the liposome solution, DSL measurements, and stability studies. The Stewart assay was conducted according to previously reported procedures [51], indicating a calculated total lipid concentration of 10.1 mmol/L. In addition, dynamic light scattering (DLS) studies revealed the size range and % polydispersity (Pd) of the liposomes (Figure 1).…”

Comprehensive review on ultrasound-responsive theranostic nanomaterials: mechanisms, structures and medical applications

“…In a similar study, calcein‐loaded liposomes functionalized with transferrin were used for the targeting of HeLa cells. Similarly, a synergistic effect between administration of LIFU and the targeting properties increased the therapeutic efficacy of the treatment [ 261 ]. A study on the concurrent use of LIFU and calcein‐loaded liposomes functionalized with human serum albumin for site-specific breast cancer therapy demonstrated similar results [ 262 ].…”

“…However, their phagocytosis in the blood circulation is still challenging [252]. Liposomes can also be targeted via surface ligands in order to maximize the efficacy of cargo delivery and minimize systemic side effects [260][261][262].…”