Aug 2026· Colloids and Surfaces B: Biointerfaces· Vol 268 Pt 2, pp.
116087
· 0 citations· 46 references
Medicine
TL;DR
The membrane damage of melanoma cells, measured by lactate dehydrogenase (LDH) assay, further supported the cytotoxic effect of Cur-ZMNs against treated cells, while showing no toxic effect against normal fibroblasts, indicating the potential of prepared Cur-ZMNs for effective treatment of melanoma.
Abstract
Treatment of melanoma is challenging due to limited bioavailability of chemotherapeutic drugs, side effects, and poor patient compliance with conventional intravenous administration. We evaluated the potential of synthesizing zein microneedles (ZMNs) using curcumin (Cur) as an anticancer model compound as a non-invasive approach for the local treatment of melanoma. A QbD approach was employed to create ZMNs with optimal mechanical strength and membrane penetrability, using zein as the matrix and PVP as a plasticizer at a concentration of 50% (w/v) and 20% (w/v), respectively. ZMNs loaded with Cur at 0.5% drug loading (Cur-ZMNs) demonstrated suitable mechanical properties, desirable membrane insertion, and sustained Cur release in vitro up to 76.17% over 24 h. Ex vivo permeation studies with excised porcine skin showed significantly higher permeation of Cur from Cur-ZMNs (59.75 %) when compared to free Cur (11%). Cur-ZMNs efficiently killed A375 melanoma cells and reduced cell viability by 44%, which was comparable to that of free Cur. The membrane damage of melanoma cells, measured by lactate dehydrogenase (LDH) assay, further supported the cytotoxic effect of Cur-ZMNs against treated cells, while showing no toxic effect against normal fibroblasts, indicating the potential of prepared Cur-ZMNs for effective treatment of melanoma.
The Zika virus (ZIKV), a neurotropic flavivirus, poses a significant global health threat due to its association with severe congenital malformations. The absence of approved antivirals necessitates novel therapeutic approaches. Curcumin, a natural polyphenol from Curcuma longa, exhibits potent anti-inflammatory and broad-spectrum antiviral properties but is plagued by poor solubility and bioavailability. This study aimed to develop and comprehensively evaluate Curcumin-loaded Solid Lipid Nanoparticles (CUR-SLNs) to overcome these limitations. A 32 factorial design optimized SLNs using glyceryl monostearate. The lead formulation (CUR-SLN6) exhibited a particle size of 53.25 nm, a high entrapment efficiency of 93.2%, and sustained in vitro release (52.89% over 24 hours). In Wistar rats, CUR-SLNs demonstrated a 15-fold increase in oral bioavailability compared to native curcumin and significant brain biodistribution. In a Vero cell-based antiviral assay, CUR-SLNs exhibited a 90% reduction in ZIKV plaque formation (IC50 = 2.5 µM), ten times more potent than native curcumin. Histopathological analysis in a lethal AG129 mouse model showed that CUR-SLN6 treatment provided marked protection against ZIKV-induced neuronal necrosis and inflammation, with efficacy comparable to Sofosbuvir. No systemic toxicity was observed. Stability studies confirmed the formulation's robustness. This study is the first to demonstrate that SLN-based delivery of curcumin not only enhances its bioavailability and brain targeting but also provides neuroprotective efficacy against ZIKV infection comparable to a direct-acting antiviral, highlighting its clinical potential as an oral neurotherapeutic agent.
R. Bhaskar, S. Saraf· Journal of drug targeting (P...· 0 citations
Chronic wounds pose a significant clinical challenge due to impaired healing, persistent inflammation, and susceptibility to infection, often by antimicrobial-resistant bacteria. Therefore, active compounds should ideally act both as antimicrobials with limited potential for resistance development and offer other beneficial wound-healing properties. Polyphenols, such as chlorogenic acid (CGA) and quercetin (QCT), exhibit those properties, but are limited by poor stability or low bioavailability.
In this study, liposomal formulations of CGA (CGA-LP) and QCT (QCT-LP) were tailored to overcome delivery barriers to wound sites. Liposomes were characterized by size, size distribution, zeta potential, entrapment efficiency, and stability.
In vitro
release studies for CGA-LP and QCT-LP demonstrated sustained payload release of ∼30% and ∼50%, respectively, over 24 h. Antioxidant activity of both compounds was assessed using DPPH and ABTS·
+
assays, confirming the radical scavenging potential of CGA comparable to vitamins C and E, while QCT showed high DPPH activity, but limited ABTS·
+
activity. Biocompatibility studies on murine macrophages revealed no cytotoxicity for either formulation. Antibacterial activity was assessed via broth microdilution for both formulations and isothermal microcalorimetry for CGA-LPs. Only QCT-LP potent measurable inhibitory effects against
Staphylococcus aureus
in the broth microdilution assay; however, effects on metabolic activity were observed for CGA-LPs. These findings suggest that liposomal entrapment could protect polyphenols and prolong or tailor their release, potentially offering a promising strategy for chronic wound therapy and addressing challenges associated with oxidative stress and bacterial infections.
L. Hemmingsen, Marte Kristensen, Cecilie Thanh Loan Dang et al.· Frontiers in Drug Delivery· 0 citations
Skin cancer is one of the most common cancers in the world, and malignant melanoma is the most aggressive and life-threatening form of skin cancer. It often quickly spreads to other parts of the body and may not always respond well to standard treatments. This calls for the urgent development of more effective and targeted treatment strategies. Protein-based nanoparticles have gained considerable attention in oncology owing to their improved bioavailability, tumour-targeted delivery potential, and reduced systemic toxicity. Silk fibroin, a versatile natural biopolymer, has emerged as a promising drug-delivery platform because of its excellent biocompatibility, biodegradability, and structural adaptability. In the present study, spherical silk fibroin-stabilised artemisinin nanoparticles (SF-ARTNPs) were synthesised and evaluated for their anti-melanoma efficacy. The developed nanoparticles demonstrated enhanced stability, improved aqueous dispersibility, high drug-loading efficiency (86.27 ± 2.05%), and a sustained drug-release profile (84.60 ± 7.29%). In vitro cytotoxicity studies revealed that SF-ARTNPs significantly reduced the viability of A375 melanoma cells to 23.31 ± 4.62% at a concentration of 40 µg mL−1, which is further corroborated by scratch assay results indicating suppressed cell migration. Collectively, these findings suggest that SF-ARTNPs have strong potential as an effective nanotherapeutic platform for treating malignant melanoma.
D. Sharda, Amanpreet Kaur, Arnab Pattanayak et al.· RSC Advances· 0 citations
Cervical cancer remains a significant global health burden, particularly in low- and middle-income countries, necessitating the development of effective localized therapeutic strategies. The present study focuses on the Quality by Design (QbD)-driven development and optimization of an apigenin-loaded chitosan-tethered in situ cubosomal gel for enhanced management of cervical cancer. Apigenin, a potent flavonoid with anticancer and anti-angiogenic properties, suffers from poor aqueous solubility and limited bioavailability, which restricts its clinical application. To overcome these limitations, cubosomal nanocarriers were formulated using glyceryl monooleate and Pluronic® F127, and optimized via central composite design (CCD) by evaluating critical quality attributes, including particle size, polydispersity index (PDI), and % entrapment efficiency. The optimized cubosomes exhibited a particle size of 253.9 nm, a low PDI of 0.06, a zeta potential of -24.4 mV, and an entrapment efficiency of 84.1 ± 1.25%, indicating a stable and efficient delivery system. Transmission electron microscopy confirmed the presence of discrete, cubic nanostructures with uniform morphology. The incorporation of cubosomes into a thermosensitive in-situ gel and surface modification with chitosan significantly improved formulation stability and enabled controlled drug release. The MTT assay revealed superior cytotoxicity of the optimized gel (IC50 = 2.753 ± 0.05 μg/mL) compared to free AGN (IC50 = 6.618 ± 0.15 μg/mL). Confocal microscopy confirmed improved cellular uptake, and the CAM assay demonstrated significant antiangiogenic activity via VEGF/HIF-1α suppression. These findings highlight the potential of CHT-AGN-CB-gel as a promising localized delivery platform for cervical cancer management, offering sustained release and reduced systemic toxicity.
Muskaan Sharma, Devesh Kumar, Mohit Kumar et al.· International Journal of Bio...· 0 citations
Non-melanoma skin cancer is one of the most frequent tumors, ranking as the fifth most common cancer. Photodynamic therapy is a noninvasive therapeutic option that involves the topical application of photosensitizers. In this context, curcumin, a polyphenolic compound extracted from Curcuma longa L., emerges as a safe alternative because of its potential phototoxic activity; however, it presents limitations such as poor skin penetration upon topical application and photodegradation. Among the promising strategies, the development of lipid nanoparticles, which are biocompatible and versatile systems, is noteworthy. In the present study, three curcumin lipid nanoparticles (LNPs) were developed and characterized, containing oleic acid, super refined castor oil, Phosal 50SA®, and Phosal 50PG® in PBS buffer, with 1.5% Poloxamer 407. The formation of these liquid crystalline phases was investigated. The LNPs exhibited mean particle sizes of 176 ± 6 nm(A1Cur), 169 ± 9 nm(C2Cur), 189 ± 19 nm(H3Cur), with corresponding PDIs of 0.133 ± 0.034; 0.226 ± 0.022 and 0.196 ± 0.009, and zeta potentials of -33 ± 1 mV; -26 ± 2 mV; -24 ± 2 mV for A1Cur, C2Cur and H3Cur, respectively. The encapsulation efficiency (EE%) was 89 ± 5% for A1Cur, 84 ± 6% for C2Cur, and 69 ± 6% for H3Cur, respectively. Small angle X-ray scattering (SAXS) revealed that only A1Cur exhibited a hexagonal liquid-crystalline phase morphology. In terms of in vitro skin penetration, A1Cur, C2Cur, and free curcumin exhibited transdermal effects, while H3Cur demonstrated greater topical potential. In ROS photogeneration assays, photoproduction was detected, particularly for LNP H3Cur. In vitro 24-hour cytotoxicity and phototoxicity against the A431 tumor cell line demonstrated that the cytotoxic and phototoxic effects were enhanced by the LNPs compared to free curcumin, especially for A1Cur. The liquid crystalline nanodispersions A1 and A1Cur were selected for incorporation into the dissolving microneedle systems, exhibiting good insertion capability and mechanical resistance to pressure. The LNPs demonstrated skin penetration potential and enhanced phototoxic and cytotoxic effects on a non-melanoma skin carcinoma cell line compared to free curcumin, highlighting the potential of these nanosystems as drug delivery vehicles for the treatment of non-melanoma cancer.
Ana Carolina Viana de Oliveira Lima, Victória Meira Holanda, Mateus Rebouças Mazza et al.· International journal of pha...· 0 citations
Histopathological and toxicity studies confirm the antiproliferative effects and safety of the transdermal LLT formulation and support the potential of transdermal LLT formulation to be an effective and safe treatment for BC.
Naifa Alenazi, Z. Khired, Hussam M Shubaily et al.· Journal of liposome research· 0 citations
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