Pharmaceutical Nanotechnology - Volume 13, Issue 2, 2025

Nanostructured lipid carriers (NLCs) are lipid-based nanoparticles composed of a mixture of solid and liquid lipids, which are stabilized by the outer surface of a surfactant.

This research aimed to prepare intranasal nanostructured lipid carriers loaded with amisulpride to enhance its dissolution and bioavailability using different formulation compositions.

Amisulpride nanostructured lipid carriers were formulated using ultra-sonication methods. Solid lipids like stearic acid, palmitic acid, and glyceryl monostearate were used, while liquid lipids like oleic acid, Imwitor 988, and isopropyl myristate were employed. Surfactants used were cremophor^®EL, tween 80, and span 20 with different co-surfactants: Transcutol HP, triacetin, and propylene glycol in different ratios. The key metrics used in this study's evaluation were particle size, polydispersity index, zeta potential, entrapment efficiency, and loading efficiency. The formulations with the best characteristics were also subjected to an in-vitro release test.

The results showed a significant shift in some evaluation criteria with a non-significant change in other characterizations upon switching between different types and ratios of compositions. A biphasic release pattern was also observed. The optimum formula F19 was found to have 68.309±0.38 nm, 0.2408±0.004, -20.64±0.11 mV, 95.75±0.26 and 18.07±0.36, respectively. It was safe on the sheep nasal membrane.

The right combination of the formulation compositions based on studying the effect of each factor on the main formulation characteristics can serve as the basis for a successful intranasal amisulpride-loaded nanostructured lipid carrier.

This study aimed to develop an anti-aging nanoformulation with Curcuma heyneana extract as bioactive substance.

Curcuma heyneana Valeton & Zipj extract has been proven in previous research to have antioxidant, anti-ageing, anti-inflammatory, and wound healing properties, which makes it a potential bioactive material for anti-ageing and sunscreen cosmetic products. Phytoantioxidants need to penetrate into deeper skin layers to ensure effectivity. Thus, a transdermal delivery system is needed to deliver the extract to a deeper skin layer.

The objective of the study was to compare the permeability and anti-ageing activity of liposomal and ethosomal formulations of C. heynena rhizome ethanolic extract.

In this study, C. heyneana extract was loaded into a phospholipid vesicular system in the form of liposome and ethosome formulations using the ethanolic injection method. The anti-ageing activity was assessed by analyzing the epidermal thickness, number of sunburn cells, distance between collagen fibers, and number of fibroblasts. While the histologic specimen scoring was carried out for the in vivo penetration study.

The ethosomal formulation had been found to have better penetration ability since it was able to reach the lower dermis area compared to the liposomes, which only reached the upper dermis. The ethosomal formulation of C. heyneana extract exhibited a better anti-ageing activity based on the parameters of epidermal thickness, sunburn cell count, fibroblast count, and the distance between collagen fibres in rat skin histology.

Ethosomes have been found to be a more proficient carrier system for transdermal delivery of C. heyneana extract compared to liposomes. Meanwhile, their penetration correlated with the effectivity of the formulation, suggesting that the vesicular system enhanced the penetration ability of the extract.

Paraquat (PQ) is an effective herbicide which is widely used around the world to remove weeds in agriculture. As a water-soluble carotenoid, crocin is a pharmacologically active constituent of C. sativus L. (saffron).

In the present study, we investigated the effects of crocin-loaded niosomes (Cro-NIO) compared to free crocin on PQ-induced toxicity in the eukaryotic human embryonic kidney (HEK293) cell line.

The Cro-NIO was synthesized and characterized. Cell viability was determined using the MTT assay in PQ-exposed HEK293 cell lines. The activities of biochemical markers were quantitatively determined to reveal the potential mechanism of PQ-induced oxidative stress in HEK293 cell line.

The particle size, zeta potential, polydispersity index (PDI), DL, and EE of Cro-NIO were 145.4 ± 19.5 nm, -22.3 ± 3.11 mV, 0.3 ± 0.03, 1.74 ± 0.01%, and 55.3 ± 7.1%, respectively. PQ-treated HEK293 cell lines decreased cell viability. The results of oxidative status showed that PQ significantly could increase ROS accumulation, accompanied by a decreasing antioxidant defense system. However, treatment with Cro-NIO, compared to crocin, not only did dose-dependently improve the cell viability but also significantly attenuated the ROS accumulation and increased antioxidant markers.

According to these results, Cro-NIO, compared to crocin, was superior to ameliorating PQ-induced cytotoxicity and oxidative damage in HEK293 cells.

Rheumatoid arthritis is indeed a constant, progressive autoimmune disease that acts on the synovial membrane, distinguished by joint pain, swelling, and tenderness. Sulfasalazine belongs to BCS Class IV having low solubility and low permeability. To overcome the issue and provide a localized effect Cubosomes were chosen for the transdermal drug delivery system.

The primary objective of this investigation was to pass on sulfasalazine-loaded cubosomes over the skin to treat rheumatoid arthritis. On the way to overcome this issue of oral sulfasalazine and provide localized effect, Cubosomes were chosen for the transdermal drug delivery system.

Sulfasalazine-loaded cubosomes were prepared by the top-down method using GMO and Poloxamer 407. Different concentrations of lipid and surfactant were used in the formulation using 3² full factorial designs. The prepared formulations were assessed for p.s, z,p, %EE, FTIR, SEM, in-vitro release, ex-vivo permeation, and deposition studies with pH 7.4 phosphate buffer saline.

The particle size varies between 65 nm to 129 nm, while the negative zeta potential ranged from -18.8 mV to -24.8 mV. The entrapment efficiency was between 87% and 95%. The formulations' in-vitro drug release was carried out for 12 hours. The optimized formulation showed a controlled release of sulfasalazine and better ex-vivo permeation and deposition properties than sulfasalazine suspension.

Overall study findings support the possibility of applying transdermal sulfasalazine-loaded cubosomes to alleviate rheumatoid arthritis.

Gold nanoparticles (GNP) have been used extensively in cancer biologics and as drug carrier systems for improved pharmacokinetics and effective therapeutic action. GNPs also ensure reliable diagnosis with sensitive imaging.

This study aimed to synthesize tizanidine hydrochloride (TZN)-biodegradable gold (Au) nanoparticles by the reduction of chloroauric acid (HAuCl4) with trisodium citrate using a microwave synthesizer and quality by design approach.

The formulation method used was optimized using a 3² (two-factor, three-level design) factorial experiment. Temperature (X1) and concentration of gold salt (X2) were the two independent factors, and particle size (Y1), Percent drug entrapment efficiency (Y2), and polydispersity index (Y3) were the responses recorded for the study.

The results of the study revealed that the optimized nanoparticles (TGN8) had a particle size (Y1) of 195 ± 1.2 nm, a polydispersity index of 0.2, and entrapment efficiency of 99.0 ± 2.9% at an optimized concentration of 14 mM gold salt (X1) and 100°C temperature (X2). Atomic Force Microscopy showed the spherical shape particles. In vitro drug release was found to be 62.1 ± 0.5% release of TZN in simulated gastric buffer (pH 1.2) and 45.5 ± 2.8% in physiological buffer (pH 7.4).

Overall, the study identified the optimal formulation conditions for TZN GNPs by considering the effects of independent variables on desired responses.

This study investigated the potential of Plant-Derived Exosome-Like Nanoparticles (PDENs) as cosmeceutical nanocarriers for treating skin problems, such as scar removal, face rejuvenation, anti-aging, and anti-pigmentation.

Researchers isolated PDENs from Yam Bean (Pachyrhizus erosus) using PEG-based precipitation, gradual filtration, and various centrifugations at low temperatures. Followed by in vitro and in vivo studies using HDF cells and Zebrafish.

The morphology of the YB-PDENs was determined using TEM analysis, they had a spherical shape with diameters of 236,83 ± 9,27 nm according to PSA. The study found that YB-PDENs were stable in aquabidest at 4°C for one month of storage and had ~-26,5 mV of Zeta Potential. The concentration of YB-PDENs was measured using the BCA Assay, and internalization of YB-PDENs to HDF cells was observed using a Confocal Laser Scanning Microscope labelled with PKH67.

As for cytotoxicity, after 24 and 72 hours of incubation with YB-PDENs, the viability of HDF cells remained more than 80%. The study also examined cell migration using the Scratch Assay and found that at 2,5 μg/mL, YB-PDENs had better migration results than other concentrations. Immunocytochemistry showed that collagen expression was higher after 14 days of incubation with YB-PDENs, and melanocytes in zebrafish decreased at each concentration compared with controls.

In conclusion, this study is the first to extract and describe PDENs from Yam Bean (Pachyrhizus erosus), with YB-PDENs having a promising anti-melanogenic effect in skin treatment. This study highlights the potential of YB-PDENs as a promising alternative to depigmentation and skin whitening treatments.

This research aimed to study the potential of PDEN from P. peruviana fruits (PENC) for regenerating and remodeling HDF.

Large wounds are dangerous and require prompt and effective healing. Various efforts have been undertaken, but have been somewhat ineffective. Plant-derived exosome-like nanoparticles (PDEN) are easily sampled, relatively cost-effective, exhibit high yields, and are non-immunogenic.

The objective of the study was to isolate and characterize PDEN from Physalis peruviana (PENC), and determine PENC’s internalization and toxicity on HDF cells, PENC's ability to regenerate HDF (proliferation and migration), and PENC ability’s to remodel HDF (collagen I and MMP-1 production).

PENC was isolated using gradual filtration and centrifugation, followed by sedimentation using PEG6000. Characterization was done using a particle size analyzer, zeta potential analyzer, TEM, and BCA assay. Internalization was done using PKH67 staining. Toxicity and proliferation assays were conducted using MTT assay; meanwhile, migration assay was carried out by employing the scratch assay. Collagen I production was performed using immunocytochemistry and MMP-1 production was conducted using ELISA.

MTT assay showed a PENC concentration of 2.5 until 500 µg/mL and being non-toxic to cells. PENC has been found to induce cell proliferation in 1, 3, 5, and 7 days. PENC at a concentration of 2.5, 5, and 7.5 µg/mL, also accelerated HDF migration using the scratch assay in two days. In remodeling, PENC upregulated collagen-1 expression from day 7 to 14 compared to control. MMP-1 declined from day 2 to 7 in every PENC concentration and increased on day 14. Overall, PENC at concentrations of 2.5, 5, and 7.5 µg/mL induced HDF proliferation and migration, upregulated collagen I production, and decreased MMP-1 levels.

Isolated PENC was 190-220 nm in size, circular, covered with membrane, and its zeta potential was -6.7 mV; it could also be stored at 4°C for up to 2 weeks in aqua bidest. Protein concentration ranged between 170-1,395 µg/mL. Using PKH67, PENC could enter HDF within 6 hours. PENC was non-toxic up to a concentration of 500 µg/mL. Using MTT and scratch assay, PENC was found to elevate HDF proliferation and migration, and reorganize actin. Using immunocytochemistry, collagen I was upregulated by PENC, whereas MMP-1 concentration was reduced.

Clove (Syzygium aromaticum) essential oil (CO) has been studied extensively for its antioxidant properties but faces several limitations, including high volatility, low aqueous solubility, and irritation.

We aimed to develop a Nanostructured Lipid Carrier (NLC) to enhance the benefits of CO.

Using the emulsification sonication method, a liquid lipid component, surfactant concentration, and a co-surfactant were optimized to create CO-loaded NLC (CO-NLC). The developed CO-NLC was rigorously assessed for its stability during storage. Free radical scavenging activity and fibroblast oxidative stress protection were also measured to assess the antioxidant activity.

The CO-NLC displayed a spherical shape with a hydrodynamic diameter of 125.77 ± 29.68 nm, homogenous particle distribution with polydispersity index of 0.26 ± 0.09, and a surface charge of -27.30 ± 4.56 mV with an encapsulation efficiency of 97% and a good stability profile. Furthermore, free CO and CO-NLC displayed very strong free radical scavenging activity with the IC50 value of 22.74 ± 0.57 µg/mL and 18.28 ± 2.63 µg/mL, respectively. However, only CO-NLC managed to protect fibroblast cells from the harmful effects of oxidative stress.

The NLC formulations improved free radical scavenging activity and effectively protected fibroblasts from oxidative stress compared to free CO.