Lipid Carriers Research Articles

Recent advancements in lipid nanoparticle technology for oral insulin delivery

Nanotechnology is important in many industries, particularly in drug delivery and administration. This technology has been used to create nanocarriers for enteral drug delivery. There are different types of nanocarriers including polysaccharide-based and lipid-based nanocarriers. Lipid nanoparticles have recently been developed for loading and administering insulin via the enteral route to treat diabetes mellitus. Insulin cannot be administered orally due to its low bioavailability, extreme gastrointestinal conditions, and instability. When insulin is loaded onto these nanocarriers, it increases bioavailability, stability, drug release pattern control, and protects insulin from extreme conditions. This review article aims to discuss recent applications as well as novel methods and approaches for oral insulin delivery using liposomes, solid lipid nanoparticles, and nanostructured lipid carriers.

Rft1 catalyzes lipid-linked oligosaccharide translocation across the ER membrane

The eukaryotic asparagine (N)-linked glycan is pre-assembled as a fourteen-sugar oligosaccharide on a lipid carrier in the endoplasmic reticulum (ER). Seven sugars are first added to dolichol pyrophosphate (PP-Dol) on the cytoplasmic face of the ER, generating Man5GlcNAc2-PP-Dol (M5GN2-PP-Dol). M5GN2-PP-Dol is then flipped across the bilayer into the lumen by an ER translocator. Genetic studies identified Rft1 as the M5GN2-PP-Dol flippase in vivo but are at odds with biochemical data suggesting Rft1 is dispensable for flipping in vitro. Thus, the question of whether Rft1 plays a direct or an indirect role during M5GN2-PP-Dol translocation has been controversial for over two decades. We describe a completely reconstituted in vitro assay for M5GN2-PP-Dol translocation and demonstrate that purified Rft1 catalyzes the translocation of M5GN2-PP-Dol across the lipid bilayer. These data, combined with in vitro results demonstrating substrate selectivity and rft1∆ phenotypes, confirm the molecular identity of Rft1 as the M5GN2-PP-Dol ER flippase.

Assessment of ex-vivo intestinal permeability and lymphatic uptake of curcumin and piperine-loaded nanostructured lipid carriers

Assessment of ex-vivo intestinal permeability and lymphatic uptake of curcumin and piperine-loaded nanostructured lipid carriers

The effect of physical stability and modified gastrointestinal tract behaviour of resveratrol-loaded NLCs encapsulated alginate beads.

Nanostructured lipid carriers (NLC) have low storage and gastrointestinal stability, limiting their applicability. The work aimed to elevate the stability and behaviour of NLC in the alimentary tract by creating an alginate bead. Through the extrusion dropping procedure, Resveratrol (RES)-loaded NLC were efficiently integrated into alginate beads. The incorporation had no significant impact on the particle size, morphology, or inner structure of NLC, as assessed using DLS (Dynamic Light Scattering), SEM (Scanning Electron Microscopy), Differential Scanning Calorimetry (DSC) and FT-IR (Fourier Transform Infra-Red). Incorporating NLC into alginate beads improves its physical stability compared to dispersion of NLC as well as NLC-Sol. An in vitro release investigation found that the NLC-alginate beads released RES more slowly than optimized NLC formulation (RES-NLCs-opt) and NLC-alginate sol. Research on simulated in vitro digestive models revealed that just a small amount of integrated NLC may permeate stomach fluid due to its tiny size. The slow diffusion of NLC from alginate to intestinal fluid prevented aggregation and allowed for gentle hydrolysis of the lipid matrix. Incorporating NLC in alginate beads shows promise for improving stability, modifying gastrointestinal behaviour, and controlling release throughout the process of digestion.

A Critical Review on the Bioavailability Promotion of the Food Bioactive Compounds: Nano Lipid Carriers Perspective

Currently, a large number of people favor meals that are rich in nutraceuticals and phytochemical compounds, which help with the treatment or prevention of chronic diseases. Oral bioavailability is a crucial component of phytochemical bioefficiency, and endogenous mechanisms have a significant impact on how well nutraceuticals and phytochemicals are absorbed by the body. In addition to endogenous variables, exogenous factors that impact the bioavailability of bioactives include the food matrix, food processing, and food storage. Different delivery systems have evolved in this regard, and nanoscale delivery tools have also been created. Delivery methods that use nanostructured lipid carriers show benefits such as enhanced loading capacity, solubility, encapsulation effectiveness, storage stability, bioavailability, and half-life. They also provide safe food systems and regulated release. In this review, the outcomes of recent experimental reports are comprehensively reviewed. In addition, the food processing, storage, gut milieu circumstances, the release process from the food and nano delivery systems in the gastrointestinal tract (GIT) milieu, interactions with other GIT constituents, main delivery systems based on nanostructured lipid carriers for their encapsulation and eventually encapsulating technological barriers, food safety concerns, and regulatory issues of nutraceutical and phytochemical compounds are discussed.

Enhancing Bovine Embryo Development In Vitro Using Oil-in-Water Nanoemulsions as Specific Carriers for Essential Lipids.

Worldwide meat consumption and production have nearly quintupled in the last 60 years. In this context, research and the application of new technologies related to animal reproduction have evolved in an accelerated way. The objective of the present study was to apply nanoemulsions (NEs) as carriers of lipids to feed bovine embryos in culture media and verify their impact on the development of embryos produced in vitro. The NEs were characterized by particle size, polydispersity, size distribution, physical stability, morphology using atomic force microscopy (AFM), surface tension, density, pH, and rheological behavior. The NEs were prepared by the emulsification/evaporation technique. A central composite rotatable design (CCRD) was used to optimize the NE fabrication parameters. The three optimized formulations used in the embryo application showed an emulsion stability index (ESI) between 0.046 and 0.086, which reflects high stability. The mean droplet diameter analyzed by laser diffraction was approximately 70-80 nm, suggesting a possible transit across the embryonic zona pellucida with pores of an average 90 nm in diameter. AFM images clearly confirm the morphology of spherical droplets with a mean droplet diameter of less than 100 nm. The optimized formulations added during the higher embryonic genome activation phase in bovine embryos enhanced early embryonic development.

Lipid-Based Nanomedicine for Alzheimer's Disease: A Comprehensive Review of Recent Advances.

Alzheimer's disease (AD) is the most common form of dementia and is expected to greatly rise in future, making it a major worldwide health concern with severe impacts on individuals and society. Despite advancements in understanding the cellular and molecular aspects of Alzheimer's disease (AD) in recent decades, it still poses a significant problem. A major problem is accurately delivering drugs to diseased neurons while minimising effects on healthy neurons. This difficulty is worsened by the low water solubility of anti-Alzheimer's disease medicines and the blood-brain barrier (BBB) that hinders the entry of central nervous system pharmaceuticals that are highly lipophilic. The focus of this article is on nanocarriers that are lipid-based. This is one of the more widely accepted methods of treating Alzheimer's disease, as it increases therapeutic efficacy while decreasing side effects related to cooperated neurological disorder payload. Searched many databases for papers published under the title (including PubMed, Elsevier, and Google Scholar). Nano Lipid Carriers (NLCs) are recognized for their ability to target the brain effectively due to their lipid-loving properties and compatibility with living tissues. They improve the absorption of drugs in the brain while decreasing the accumulation of drugs in unintended organs. This work emphasises the importance of nano lipid carriers, which are lipophilic and biocompatible and have demonstrated exceptional targeting efficiency, making them an ideal carrier system for delivering medications to the brain.

A stability indicating method development and validation of a rapid and sensitive RP-HPLC method for Nintedanib and its application in quantification of nanostructured lipid carriers.

Nintedanib (NTB) is a multiple tyrosine kinase inhibitor, been investigated for many disease conditions like idiopathic pulmonary fibrosis (IPF), systemic sclerosis interstitial lung disease (SSc-ILD) and non-small cell lung cancer (NSCLC). NTB is available as oral capsule formulation, but its ability to detect degradants formed through oxidative, photolytic and hydrolytic processes makes it difficult to quantify. In the current work, a novel reversed-phase high-performance liquid chromatography (RP-HPLC) method was developed and validated. The developed method is simple, precise, reproducible, stable and accurate. The inherent stability of NTB was evaluated using the proposed analytical method approach and force degradation studies were carried out. NTB was separated chromatographically on the Shimadzu C 18 column as stationary phase (250 ×4.6 mm, 5 µm) using an isocratic elution method with 0.1% v/v triethyl amine (TEA) in HPLC grade water and acetonitrile (ACN) in the ratio 35:65% v/v. The mobile phase was pumped at a constant flow rate of 1.0 ml/min, and the eluent was detected at 390 nm wavelength. NTB was eluted at 6.77±0.00 min of retention time (t R) with a correlation coefficient of 0.999, the developed method was linear in the concentration range of 0.5 µg/ml to 4.5 µg/ml. The recovery rate was found to be in the range of 99.391±0.468% for 1.5 µg/ml concentration. Six replicate standards were determined to have an % RSD of 0.04. The formulation excipients didn't interfere with the determination of NTB, demonstrating the specificity of the developed method. The proposed approach of the analytical method developed can be used to quantify the amount of NTB present in bulk drugs and pharmaceutical formulations.

Combined photodynamic therapy and hollow microneedle approach for effective non-invasive delivery of hypericin for the management of imiquimod-induced psoriasis

Background Conventional topical psoriasis treatments suffer from limited delivery to affected areas and skin irritation due to high local drug concentration. Purpose This study aims to prepare hypericin (HYP) loaded nanostructured lipid carriers (NLCs) and their application in psoriasis treatment through intradermal administration using hollow microneedles assisted by photodynamic therapy. Methods The colloidal characteristics of NLCs, entrapment efficiency and morphology were evaluated. An ex-vivo skin distribution study was conducted along with testing the in vivo antipsoriatic activity in mice with the imiquimod-induced psoriasis model. Results The particle size and zeta potential of HYP-NLCs were 167.70 nm and −18.1, respectively. The ex-vivo skin distribution study demonstrated the superior distribution of HYP-NLCs to a depth of 1480 µm within the skin layers relative to only 750 µm for free HYP. In vivo studies revealed that the levels of NF-KB, IL 6, MMP1, GSH, and catalase in the group treated with HYP-NLCs in the presence of light were comparable to the negative control. Conclusions The histopathological inspection of dissected skin samples reflected the superiority of HYP-NLCs over HYP ointment. This could be ascribed to the effect of nanoencapsulation on improving HYP properties besides the ability of hollow microneedles to ensure effective HYP delivery to the affected psoriatic area.

Alendronate/lactoferrin-dual decorated lipid nanocarriers for bone-homing and active targeting of ivermectin and methyl dihydrojasmonate for leukemia

Chronic myeloid leukemia is a hematological cancer, where disease relapse and drug resistance are caused by bone-hosted-residual leukemia cells. An innovative resolution is bone-homing and selective-active targeting of anticancer loaded-nanovectors. Herein, ivermectin (IVM) and methyl dihydrojasmonate (MDJ)-loaded nanostructured lipid carriers (IVM-NLC) were formulated then dually decorated by lactoferrin (Lf) and alendronate (Aln) to optimize (Aln/Lf/IVM-NLC) for active-targeting and bone-homing potential, respectively. Aln/Lf/IVM-NLC (1 mg) revealed nano-size (73.67 ± 0.06 nm), low-PDI (0.43 ± 0.06), sustained-release of IVM (62.75 % at 140-h) and MDJ (78.7 % at 48-h). Aln/Lf/IVM-NLC afforded substantial antileukemic-cytotoxicity on K562-cells (4.29-fold lower IC50), higher cellular uptake and nuclear fragmentation than IVM-NLC with acceptable cytocompatibility on oral-epithelial-cells (as normal cells). Aln/Lf/IVM-NLC effectively upregulated caspase-3 and BAX (4.53 and 15.9-fold higher than IVM-NLC, respectively). Bone homing studies verified higher hydroxyapatite affinity of Aln/Lf/IVM-NLC (1 mg; 22.88 ± 0.01 % at 3-h) and higher metaphyseal-binding (1.5-fold increase) than untargeted-NLC. Moreover, Aln/Lf/IVM-NLC-1 mg secured 1.35-fold higher in vivo bone localization than untargeted-NLC, with lower off-target distribution. Ex-vivo hemocompatibility and in-vivo biocompatibility of Aln/Lf/IVM-NLC (1 mg/mL) were established, with pronounced amelioration of hepatic and renal toxicity compared to higher Aln doses. The innovative Aln/Lf/IVM-NLC could serve as a promising nanovector for bone-homing, active-targeted leukemia therapy.

Characteristic and storage stability of nanostructured lipid carriers containing red palm oil

Red palm oil (RPO) is a potential carotenoid source mostly containing β-carotene. RPO instability requires a delivery system such as nanostructured lipid carriers (NLC). This research aimed to develop an NLC delivery system and study the characteristics of NLCRPO. The melting-emulsification-ultrasonication method was employed to produce the NLC-RPO based on 6% (w/w) lipids, with solid lipid to RPO ratio (SRR) varied 6:4, 7:3, and 8:2. Tween 80 (24% w/w) to lipids ratio of 4:1, and distilled water 70% (w/w). The solid lipids employed in this investigation were palm stearin (PS), and palm kernel stearin (PKS), while the liquid lipid was RPO. The stability of NLC-RPO was evaluated using βcarotene entrapment efficiency (EE), centrifugation, cooling, heating test, color, and pH for 90 days of storage. The NLC-RPO was characterized by particle size, polydispersity index (PDI), zeta potential, and viscosity before and after 90 days. Regression analysis was performed to evaluate the relationships between the storage and stability parameters. The highest encapsulation efficiency of β-carotene in NLC-RPO as a carrier β-carotene from the RPO was achieved when solid lipid to RPO ratio (SRR) of 6:4 and there was no significant difference in the type of solid lipid (PS and PKS) used. Generally, NLC-RPO stored for 90 days at room temperature showed good stability after centrifugation, cooling and heating tests with greenish-yellow color (-a*;+b*), and pH of 6.38-6.54. The particle size (38-87 nm), PDI (0.01-0.54), and zeta potential (-10.17 to -22.67 mV) did not significantly change over 90 days of storage, while the viscosity (8.36-9.11cP) was significantly different. The NLC-RPO with SRR of 6:4 had the highest β-carotene entrapment efficiency and remained stable after 90 days of storage at room temperature.

D-α-tocopheryl polyethylene glycol succinate-decorated dual drug-loaded lipidic nanocarriers: A strategic approach for targeting lymphatic uptake and p-gp efflux modulation to enhance oral bioavailability in HIV-1 viral reservoirs

The toxicity potential and inadequate bioavailability of antiretroviral therapy restrict their effectiveness in completely eradicating HIV-1 from viral reservoirs, as the drugs encounter difficulties in accessing these reservoirs. This study presents a combinatorial d-α-tocopheryl polyethylene glycol succinate (TPGS)-decorated nano-structured lipid carrier of Etravirine (ETR) and Darunavir Ethanolate (DRVE) that was formulated, optimized, and characterized to achieve synergistic effects against HIV-1 infection. The effectiveness of the combinatorial approach was evaluated by in silico studies, and their docking score and free binding energy showed that both drugs demonstrate synergistic effects against their respective enzymes. The cellular research of ED (ETR and DRVE) in TMZ-b1 cell lines also showed that the best ratio of ETR and DRVE (1:6.5 μg/mL) produced a combined effect. The formulation, termed ED-TPGS-NLCs, underwent optimization using central composite rotational design (CCRD) through a modified emulsification process, followed by characterization based on globule size, polydispersity index (PDI), percentage entrapment efficiency, percentage drug loading, and transmission electron microscopy (TEM) analysis. In vitro release studies demonstrated a notable improvement of drug release from the optimized lipid nanosystem, conforming to the Korsmeyer-Peppas kinetics model. Besides, the in-vitro studies, the intestinal permeation enhancement study, the intestinal depth analysis, and the pharmacokinetic assessment of the optimized formulation in Wistar rats were performed to improve permeation and increase plasma drug concentration. ED-TPGS-NLCs also stopped HIV-1 infection in TMZ-b1 cell lines by 50 %, and the lowest concentration needed to do this was about 58 times lower than purified ED suspension. These studies ensure that ED-TPGS-NLCs were taken up due to the formation of chylomicrons and inhibit the p-gp efflux system by TPGS and solutol to inhibit the first-pass hepatic metabolism, which helps to improve the intestinal permeation and enhance plasma drug concentration, leading to enhanced oral bioavailability of ED. Hence, the improved bioavailability of ED in the nanoformulation also enhanced the anti-retroviral efficacy and improved the safety margins of ED-TPGS-NLCs. These findings can also reduce the side effects of high doses of antiretroviral drugs.

In vitro and in vivo studies of ocular topically administered NLC for the treatment of uveal melanoma

Uveal melanoma is one of the most common and aggressive intraocular malignancies, and, due to its great capability of metastasize, it constitutes the most incident intraocular tumor in adults. However, to date there is no effective treatment since achieving the inner ocular tissues still constitutes one of the greatest challenges in actual medicine, because of the complex structure and barriers. Uncoated and PEGylated nanostructured lipid carriers were developed to achieve physico-chemical properties (mean particle size, homogeneity, zeta potential, pH and osmolality) compatible for the ophthalmic administration of (S)-(–)-MRJF22, a new custom-synthetized prodrug for the potential treatment of uveal melanoma. The colloidal physical stability was investigated at different temperatures by Turbiscan® Ageing Station. Morphology analysis and mucoadhesive studies highlighted the presence of small particles suitable to be topically administered on the ocular surface. In vitro release studies performed using Franz diffusion cells demonstrated that the systems were able to provide a slow and prolonged prodrug release. In vitro cytotoxicity test on Human Corneal Epithelium and Human Uveal Melanoma cell lines and Hen’s egg-chorioallantoic membrane test showed a dose-dependent cytotoxic effect of the free prodrug on corneal cells, whose cytocompatibility improved when encapsulated into nanoparticles, as also confirmed by in vivo studies on New Zealand albino rabbits. Antiangiogenic capability and preventive anti-inflammatory properties were also investigated on embryonated eggs and rabbits, respectively. Furthermore, preliminary in vivo biodistribution images of fluorescent nanoparticles after topical instillation in rabbits’ eyes, suggested their ability to reach the posterior segment of the eye, as a promising strategy for the treatment of choroidal uveal melanoma.

On the Structure, Stability, and Cell Uptake of Nanostructured Lipid Carriers for Drug Delivery.

The efficacy of nanostructured lipid carriers (NLC) for drug delivery strongly depends on their stability and cell uptake. Both properties are governed by their compositions and internal structure. To test the effect of the lipid composition of NLC on cell uptake and stability, three kinds of liquid lipids with different degrees of unsaturation are employed. After ensuring homogeneous size distributions, the thermodynamic characteristics, stability, and mixing properties of NLC are characterized. Then the rates and predominant pathways of cell uptake are determined. Although the same surfactant is used in all cases, different uptake rates are observed. This finding contradicts the view that the surface properties of NLC are dominated by the surfactant. Instead, the uptake rates are explained by the structure of the nanocarrier. Depending on the mixing properties, some liquid lipids remain inside the nanocarrier, while other liquid lipids are present on the surface. Nanocarriers with liquid lipids on the surface are taken up more readily by the cells. This shows that the engineering of efficient lipid nanocarriers requires a delicate balance of interactions between all components of the nanocarrier on the molecular level.

Effect of Cremophor RH40, Hydroxypropyl Methylcellulose, and Mixing Speed on Physicochemical Properties of Films Containing Nanostructured Lipid Carriers Loaded with Furosemide Using the Box-Behnken Design.

This study aimed to examine the characteristics of H-K4M hydroxypropyl methylcellulose (HPMC) films containing nanostructured lipid carriers (NLCs) loaded with furosemide. A hot homogenization technique and an ultrasonic probe were used to prepare and reduce the size of the NLCs. Films were made using the casting technique. This study used a Box-Behnken design to evaluate the influence of three key independent variables, specifically H-K4M concentration (X1), surfactant Cremophor RH40 concentration (X2), and mixing speed (X3), on the physicochemical properties of furosemide-loaded NLCs and films. The furosemide-loaded NLCs had a particle size ranging from 54.67 to 99.13 nm, and a polydispersity index (PDI) ranging from 0.246 to 0.670. All formulations exhibited a negative zeta potential, ranging from -7.05 to -5.61 mV. The prepared films had thicknesses and weights ranging from 0.1240 to 0.2034 mm and 0.0283 to 0.0450 g, respectively. The drug content was over 85%. Film surface wettability was assessed based on the contact angle, ranging from 32.27 to 68.94°. Film tensile strength varied from 1.38 to 7.77 MPa, and their elongation at break varied from 124.19 to 170.72%. The ATR-FTIR analysis confirmed the complete incorporation of the drug in the film matrix. Therefore, the appropriate selection of values for key parameters in the synthesis of HPMC films containing drug-loaded NLCs is important in the effective development of films for medical applications.

A Comprehensive Review of the Use of Nanoparticles in Cosmeceutical Science

Nanotechnology is significantly impacting the cosmeceutical sector, revolutionizing how skincare products are formulated and delivered. Innovative nanoparticle delivery systems such as liposomes, niosomes, nanostructured lipid carriers (NLCs), solid lipid nanoparticles (SLNs), gold nanoparticles, and nano-emulsions are at the forefront of this transformation. These systems enhance the bioavailability, stability, and efficacy of active ingredients, offering controlled release and targeted delivery features that are crucial for optimizing cosmetic results. Nanotechnology facilitates improved penetration of actives into the skin, protects ingredients from degradation, and ensures sustained release, thereby enhancing the therapeutic effectiveness of cosmeceuticals. Additionally, the integration of nanoparticles into cosmetic products allows for reduced dosages and minimized side effects, which contributes to better skin tolerance and safety. However, the use of nanotechnology in cosmeceuticals is not without challenges. It raises significant safety and environmental concerns due to the potential systemic absorption of nanoparticles. Regulatory bodies globally are striving to address these issues, with guidelines and regulations continuously evolving to ensure consumer safety while fostering innovation. The current review highlights the dual aspects of opportunity and oversight that nanotechnology brings to the beauty and skincare industry, emphasizing the need for ongoing research and regulatory vigilance to harness its full potential responsibly

Box-Behnken Design-Based Optimization and Evaluation of Lipid-Based Nano Drug Delivery System for Brain Targeting of Bromocriptine.

Bromocriptine (BCR) presents poor bioavailability when administered orally because of its low solubility and prolonged first-pass metabolism. This poses a significant challenge in its utilization as an effective treatment for managing Parkinson's disease (PD). The utilization of lipid nanoparticles can be a promising approach to overcome the limitations of BCR bioavailability. The aim of the research work was to develop and evaluate bromocriptine-loaded solid lipid nanoparticles (BCR-SLN) and bromocriptine-loaded nanostructured lipid carriers (BCR-NLC) employing the Box-Behnken design (BBD). BCR-SLNs and BCR-NLCs were developed using the high-pressure homogenization method. The prepared nanoparticles were characterized for particle size (PS), polydispersity index (PDI), and entrapment efficiency (EE). In vitro drug release, cytotoxicity studies, in vivo plasma pharmacokinetic, and brain distribution studies evaluated the optimized lipid nanoparticles. The optimized BCR-SLN had a PS of 219.21 ± 1.3 nm, PDI of 0.22 ± 0.02, and EE of 72.2 ± 0.5. The PS, PDI, and EE of optimized BCR-NLC formulation were found to be 182.87 ± 2.2, 0.16 ± 0.004, and 83.57 ± 1.8, respectively. The in vitro release profile of BCR-SLN and BCR-NLC showed a biphasic pattern, immediate release, and then trailed due to the sustained release. Furthermore, a pharmacokinetic study indicated that both the optimized BCR-SLN and BCR-NLC formulations improve the plasma and brain bioavailability of the drug compared to the BCR solution. Based on the research findings, it can be concluded that the BCR-loaded lipid nanoparticles could be a promising carrier by enhancing the BBB penetration of the drug and helping in the improvement of the bioavailability and therapeutic efficacy of BCR in the management of PD.

Lipid-based Nanocarrier Drug Delivery Approach for Biomedical Application

Abstract: The development of nanosized drug-carrier systems has been investigated over the past few decades using various techniques. The two main categories of these systems are polymeric nanoparticles and lipid nanoparticles (LNPs). The toxicological risk associated with lipid nanoparticles is significantly lower than the danger associated with polymeric nanoparticles due to the materials' natural and biological origins. Lipid-based drug delivery systems like Nanostructured lipid carriers (NLCs) and Solid Lipid Nanoparticles (SLNs) are well-established nanotechnology systems for preparing all major pharmaceuticals. These delivery systems can be scaled up with easy manufacturing procedures and are biocompatible. NLCs are the second generation of lipid-based nanocarriers (SLNs), formed by combining solid and liquid biocompatible lipids to form an unstructured matrix that provides high entrapment efficiency of active constituents. LNPs can promote the distribution of active pharmaceutical ingredients to the target site. Increasing the active drug concentration to target organ LNPs enhances the therapeutic effectiveness and reduces the side effects. This paper reviews the structure of SLNs and different NLCs, various steps involved in manufacturing lipid nanoparticles, excipients used in the formulation, and applications for targeted drug delivery.

Application of 20(S)-Protopanaxadiol-Loaded Nanostructured Lipid Carriers for Diabetic Wound Healing and Vascular Regeneration

Chronic wounds in diabetic patients have become a common complication. However, current wound management tends to yield unsatisfactory outcomes and may give rise to complications. Therefore, we prepare a nano-structured lipid carrier by incorporating a 20(S)-Protopanaxadiol (PPD)-loaded lipid nanoparticles (PPD-N) into a silicone elastomer (PPD-NS) for treating chronic diabetic wounds and assess its therapeutic efficacy in promoting diabetic wound healing and vascular regeneration in a mouse model. Our findings revealed that the prepared PPD-N showed uniform distribution with spherical morphology and an average diameter of approximately 130 nm. Moreover, PPD-NS exhibited a wound closure rate of 92.1% after 48 hours of treatment and demonstrated enhanced vascular regeneration. Therefore, it can be concluded that the prepared PPD-NS can effectively be used in diabetic wound repair and vascular regeneration. This study provides a promising potential therapeutic option for diabetic wounds.

Development of NLC-based Sunscreen Gel of Green Tea Extract and its In vitro Characterization

Background: Green tea extract is a hydrophilic antioxidant. The challenge associated with its cutaneous administration is its poor penetration. A system of solid-liquid lipids formulated in the form of a nanostructured lipid carrier (NLC), can improve the penetration. In addition, Vitamin E oil used as a liquid lipid will aid in skin hydration, reduce particle size, and enhance penetration. Objective: The objective of this study was to formulate the NLC-based sunscreen gel of green tea extract. Methods: Nanostructured lipid carriers (NLC) were prepared by melt emulsion ultrafiltration technique and were evaluated for particle size, zeta potential, polydispersity index (PDI), drug loading (DL), encapsulation efficacy (EE), and in vitro drug release. The optimised formula was incorporated into a suitable gel base and an in-vitro sun protection factor (SPF) was determined. Beeswax and Vitamin E oil were chosen as solid and liquid lipids for NLC formulation. Results: The particle size, PDI, zeta potential, entrapment efficiency, and in vitro drug release of optimised formulation (NLC4) were found to be 139.4 nm, 0.236, -11.0 mV, 84.20%, and 85% respectively. The SPF value of green tea extract-NLC-loaded gel was found to be 20.035. Conclusion: The result of the current investigation depicted that lipid nanoparticles are suitable carriers for green tea extract to be delivered as sunscreen gel.