Current Drug Delivery - Volume 22, Issue 9, 2025

The spread of tumors (48% in men and 51% in women), as well as the protection of malignant tumors by stromal cells and complex blood vessels, pose significant challenges to drug delivery to tumors. Modern chemotherapy, on the other hand, addresses tumor growth suppression by at least 60% through versatile formulation systems and numerous modifications to drug delivery systems. The renewable and naturally occurring polymers present invariably in all living cells form the fundamental foundation for most anticancer drug development. The review aims to discuss in detail the preparations of polysaccharide, lipid, and protein-based drug-loading vehicles for the targeted delivery of prominent anticancer drugs. It also provides an explanation of drug distribution in blood (cumulative releases of nearly 80% drug) and drug accumulation at tumor sites (1–5 mg/kg) due to enhanced permeability and retention (EPR).

Specific delivery examples for treating colorectal and breast carcinomas have been presented to distinguish the varied drug administration, bioavailability, and tumor internalization mechanisms between sugar, fatty acid, and amino acid polymers. Current therapy possibilities based on cutting-edge literature are provided, along with drug delivery systems tailored to tumor location and invasive properties.

The unique combinations of the three natural polymers provide unparalleled solutions to minimize the toxicity (<20% drug release) of the chemotherapeutic drugs on normal tissues. Moreover, the development of a consolidated drug delivery system has contributed to a substantial reduction (dose reduction from 10.43 µM to 1.9 µM) in the undesirable consequences of higher dosages of chemotherapeutic drugs.

The review extensively covers safe chemotherapeutic systems with significant advantages (tumor volume shrinkage of 4T1 cells from 1000 mm³ to 200 mm³) in clinical applications of carcinoma treatments using natural polymers.

Reproducibility and scale-up production of microspheres through spray drying present significant challenges. In this study, biodegradable microspheres of Triamcinolone Acetonide Acetate (TAA) were prepared using a novel static mixing method by employing poly(lactic-co-glycolic acid) (PLGA) as the sustained-release carrier.

TAA-loaded microspheres (TAA-MSs) were prepared using a static mixing technique. The PLGA concentration, polyvinyl alcohol concentration (PVA), phase ratio of oil/water, and phase ratio of water/solidification were optimized in terms of the particle size, drug loading (DL), and encapsulation efficiency (EE) of TAA-MSs. The morphology of TAA-MSs was examined using Scanning Electron Microscopy (SEM), while the physicochemical properties were evaluated through X-ray diffraction (XRD), Differential Scanning Calorimetry (DSC), and Fourier Transform Infrared Spectroscopy (FT-IR). The in vitro release of TAA-MSs was compared to that of the pure drug (TAA) using a water-bath vibration method in the medium of pH 7.4 at 37°C.

The formulation composition and preparation condition for the preparation of TAA-MSs were optimized as follows: the PLGA concentration was 1%, the phase ratio of oil(dichloromethane) /water (PVA solution) was 1:3, the phase ratio of water (PVA solution)/solidification was 1:2. The optimized TAA-MSs displayed spherical particles with a size range of 30-70 μm, and DL and EE values of 27.09% and 98.67%, respectively. Moreover, the drug-loaded microspheres exhibited a significant, sustained release, with 20% of the drug released over a period of 28 days. The XRD result indicated that the crystalline form of TAA in microspheres had been partly converted into the amorphous form. DSC and FT-IR results revealed that some interactions between TAA and PLGA occurred, indicating that the drug was effectively encapsulated into PLGA microspheres.

TAA-loaded PLGA microspheres have been successfully prepared via the static mixing technique with enhanced EE and sustained-release manner.

Hepatocellular carcinoma (HCC) poses a major healthcare burden globally. Traditional Chinese medicine formula Bushen Jianpi (BSJP) recipe shows inhibitory effects on HCC but suffers from low bioavailability. This study aims to develop a BSJP-loaded liposome (BSJP@Lip) for targeted HCC treatment.

BSJP@Lip was prepared using a microfluidic device. Particle characterization included size, morphology, drug loading, encapsulation efficiency, and release kinetics analysis. In vitro cytotoxicity, cellular uptake, apoptosis, and protein expression were evaluated in hepG2, Smmc-7721, and hepa 1-6 hepatic cancer cell lines treated with BSJP@Lip.

BSJP@Lip nanoparticles showed a uniform spherical shape with an average size of 50 nm and zeta potential at around -2.24 mV. They significantly inhibited cell viability and induced apoptosis in a dose-dependent manner compared with traditional decoction formulations. Enhanced cellular uptake of BSJP@Lip increased the expression of proinflammatory factors IL-18 and NLRP3.

BSJP@Lip nanoparticles were found to be efficiently internalized by hepatic cancer cell lines, resulting in a dose-dependent inhibition of cell viability and induction of apoptosis. This effect was accompanied by the upregulation of IL-18 and NLRP3.

The incidence and mortality rates of liver cancer are high; therefore, developing new drug delivery systems with good biocompatibility and targeting has become a research hotspot.

Mitoxantrone hydrochloride (MH) loaded in acidic Panax notoginseng polysaccharide III nanoparticles (MANPs) was prepared using electrostatic adsorption. This was achieved by loading MH in acidic Panax notoginseng polysaccharide III (APPN III), a natural compound that exhibits anti-tumor activity. Response surface methodology was used to determine the parameters for the best formulation.

Fourier-transform infrared spectroscopy and differential scanning calorimetry indicated that MH in MANPs was amorphous and exhibited good encapsulation efficiency in the carrier. Findings from dynamic dialysis confirmed that MANPs exhibited slow drug release at pH 6.8 and over the pH range of 7.2-7.4. In vitro experiments confirmed the anti-tumor effects of MANPs on H22 cells based on the inhibition of cell proliferation and an increase in apoptosis. MANPs also demonstrated an obvious anti-tumor effect without any toxicity in H22 tumor-bearing mice. This effect could be attributed to APPN III enhancing the immune system and exerting a synergistic anti-tumor effect in combination with MH, thereby alleviating MH-induced damage to the immune system in H22 tumor-bearing mice.

As a nano-carrier prepared using natural resources, APPN III shows immense potential in the field of drug delivery and could serve as a novel option for the effective delivery of chemotherapeutic drugs.

A serious public health condition called liver fibrosis can cause cirrhosis, cancer, and even patient death.

This study sought to determine if Luteolin (LUT) and Silibinin (SBN) could protect rats against oxidative stress and liver fibrosis caused by thioacetamide (TAA) over three weeks, as well as any potential mechanisms of action. There will be 49 adult Wistar albino rats utilized, split up into 7 groups: (G1) Negative control, (G2) Positive control, (G3) LUT+TAA, (G4) SBN+TAA, (G5) mix LUT+ SBN, (G6) LUT+SBN with TAA, (G7) LUT+SBN then TAA, and so. Liver function tests and oxidative stress markers were measured after the experiment. The liver underwent microscopic inspection. Rats given TAA treatment had significantly higher liver enzymes than control; yet, albumin (ALB), total protein (TP), superoxide dismutase (SOD), and reduced glutathione (GSH) significantly decreased.

Following three weeks of TAA exposure, liver sections revealed hepatocytic damage and fibrosis. Oxidative stress, histological alterations, and alterations in liver function were all lessened in TAA rats administered with LUT, SBN, or both.

The combined hepatoprotective benefits of LUT and SBN prevented TAA-induced biochemical and histological alterations in rat liver, acting in concert with each other.

Nanofiber (NF) films have emerged as a promising alternative for treating psoriasis. Based on their specific characteristics, they have distinguished themselves from other topical dosage forms, such as hydrogels, foams, and sponges. This research looks at making biocompatible and biodegradable nanofibers out of polyvinyl alcohol (PVA) and gelatin and adding hesperidin (HPN) and ofloxacin (OFX) as medicine.

HPN-OFX-integrated nanofiber (HPN-OFXNF) films were prepared using electrospinning. Subsequently, the surface morphology, entrapment efficiency, in vitro drug diffusion, and antimicrobial, anti-inflammatory, and anti-psoriasis properties were investigated.

Scanning electron microscopy (SEM) analysis revealed that the produced nanofibers exhibited smooth surfaces with diameters from 50.67 to 114.4 nm, entrapment efficiencies from 69.3 ± 1.8% for OFX and 45.63 ± 1.6% for HPN. At the end of 48 h, nanofibers showed 90.8 ± 2.4% of OFX and 97.3± 3.1% of HPN release. In vitro, antimicrobial testing of the films demonstrated 24.89 ± 3.2 and 42.46 ± 4.4 mm zones of inhibition against E. coli and S. aureus. The total antioxidant activity of HPN is 198.67±2.38 (µ mol AAE/mg HPN), and HPN-OFXNF is 271.12 ± 3.56 (µ mol AAE/mg HPN-OFXNF), and their IC50 values against HaCaT cell growth of 80.5 ± 2.5 and 64.6 ± 3.4 µg/ml, respectively.

HPN-OFXNFs have been developed successfully by the electrospinning method with moderate entrapment efficiencies, showing a biphasic trend of an early burst trailed by a sustained pattern of drug release, depending on the surface area and diameter of the fibers. Enhanced zones of inhibition and anti-inflammatory efficacy of NFs in comparison with their pure counterparts have been demonstrated to be beneficial. Stronger antioxidant efficacy, inducing anti-proliferation and promoting apoptosis in human keratinocytes, has made them the best versions over pure drug compounds.

This therapy, which includes a combined anti-inflammatory and antibacterial treatment strategy with an innovative drug delivery system, has proven to be a promising development in treating psoriasis.