Reversed lipid-based nanoparticles dispersed in oil for malignant tumor treatment via intratumoral injection

Abstract

Intratumoral injection of anticancer drugs directly delivers chemotherapeutics to the tumor region, offering an alternative strategy for cancer treatment. However, most hydrophilic drugs spread quickly from the injection site into systemic circulation, leading to inferior antitumor activity and adverse effects in patients. Therefore, we developed novel reversed lipid-based nanoparticles (RLBN) as a nanoscale drug carrier. RLBNs differ from traditional nanoscale drug carriers in that they possess a reversed structure consisting of a polar core and lipophilic periphery, leading to excellent solubility and stability in hydrophobic liquids; therefore, hydrophilic drugs can be entrapped in RLBNs and dispersed in oil. In vivo studies in tumor-bearing Balb/c nude mice indicated remarkable antitumor activity of RLBN-DOX after a single injection, with effective tumor growth inhibition for at least 17 days; the inhibition rate was $80%. These results can be attributed to the long-term retention and sustained drug release of RLBN-DOX in the tumor region. In contrast, intratumoral injection of free DOX showed weaker antitumor activity than RLBN-DOX did, with the tumor size doubling by day 11 and tripling by day 17. Further, the initial burst of drug released from free DOX could produce detrimental systemic effects, such as weight loss. Histological analyses by TUNEL staining showed apoptosis after treatment with RLBN-DOX, whereas tumor cell viability was high in the free DOX group. Current results indicate that RLBNs show sustained delivery of hydrophilic agents to local areas resulting in therapeutic efficacy, and they may be a promising drug delivery system suitable for intratumoral chemotherapy. ARTICLE HISTORY

Lipopolysaccharide-coated CuS nanoparticles promoted anti-cancer and anti-metastatic effect by immuno-photothermal therapy

“…When considering the cost-effectiveness, CuS is the ideal material as its performance in treatment is not limited by the worth of the laser source, meaning that it can satisfactorily exhibit the photothermal effect under the irradiation of 808 nm laser, known as a readily accessible optical instrument. In addition, as keeping abreast of trend, the excuse for intratumoral injection of LPS-CuS without any targeting aspect, instead of intravenous injection, is not only to prevent the unexpected side effects, but also maximize the therapeutic effect through the intensified delivery of photothermal effect and anti-cancer effect [ 40 ].…”

“Oil-soluble” Reversed Lipid Nanoparticles for Oral Insulin Delivery

“…Our previous study showed that water-soluble drugs can be e ciently encapsulated into ORLN using a simple three-step technique [13,14]. In this study, 200 μg/mL ORLN-PHI oil solution was successfully formed by dissolving the lyophilized dry cake in MCT.…”

“…Our recent study reported a technique to encapsulate and "dissolve" water-soluble chemotherapeutic agents into vegetable oil by forming "oil-soluble" reversed lipid nanoparticles (ORLN) [13,14]. This carrier can either decrease the intestinal hydrolytic degradation of topotecan (TPT) via protection by both a phospholipid (PC) shell and oil medium, or improve the oral absorption of TPT by enhancing the intestinal lymphatic transport.…”

Taste masking of water-soluble drug by solid lipid microspheres: a child-friendly system established by reversed lipid-based nanoparticle technique

“…Atomoxetine hydrochloride‐reversed lipid‐based nanoparticles were prepared as previously described (Shen et al [20] …”

“…We have reported that reversed lipid‐based nanoparticles (RLBNs) can solubilize hydrophilic drugs in liquid oil by forming a core‐shell structure [19–21] . Biocompatible phospholipids are important materials in RLBNs.…”