Advances in Capsaicin-Based Nanocarriers: Bridging Mechanistic Insights with Therapeutic Potential and Clinical Outcomes.

Objective This review aims to evaluate the therapeutic potential of Risperidone (RSP)-loaded nanoparticles as an innovative drug delivery approach for effective schizophrenia (SZ) management and improved patient outcomes. Significance Schizophrenia is a long-standing mental disorder involving disturbances in thought, perception, and behavior, frequently necessitating extended pharmacologic therapy. While RSP, a second-generation antipsychotic, is efficacious against both positive and negative symptoms, its therapeutic use is impaired by limited water solubility, low oral bioavailability, extensive first-pass metabolism, and dose-dependent side effects. Overcoming these limitations may substantially benefit patient outcomes. Recent advances in nanotechnology have allowed the development of several RSP-loaded nanocarriers such as polymeric nanoparticles, solid lipid nanoparticles, and nanostructured lipid carriers. Key findings This review evaluates these systems according to drug loading efficiency, release kinetics, brain-targeting capacity, and drug administration routes, according to preclinical data. RSP nanoparticles exhibited improved solubility, sustained release, enhanced brain targeting, and decreased systemic toxicity. Intranasal and parenteral routes are additional advantages in enhancing bioavailability and compliance in non-compliant patients. Such formulations provide improved pharmacokinetic profiles and reduce extrapyramidal symptoms. Conclusion RSP-loaded nanoparticles are a valuable innovation in SZ therapy through enhancing efficacy, minimizing side effects, and improving patient compliance. More clinical studies are warranted to determine their safety, long-term efficacy, and commercial viability for translation into the clinic.

Are nanostructured lipid carriers (NLCs) better than solid lipid nanoparticles (SLNs): Development, characterizations and comparative evaluations of clotrimazole-loaded SLNs and NLCs?

The objective of this study was to develop and evaluate solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) utilizing sucrose ester as a stabilizer/emulsifier for the controlled release of drug/active. Both SLNs and NLCs were prepared using different sugar esters to screen out the most suitable stabilizer. Clotrimazole was used as a model active/drug. The effect of different formulation variables on the particle size, polydispersity index and drug encapsulation efficiency of SLNs and NLCs was evaluated and compared. SLNs and NLCs were physicochemically characterized and compared using Cryo-SEM, DSC and XRD. Furthermore, a drug release study of SLNs and NLCs was conducted. Finally, physicochemical stability (size, PI, ZP, EE) of the SLNs and NLCs was checked at 25 ± 2 °C and at 2–8 °C. Among the sucrose esters, D-1216 was found to be most suitable for both SLNs and NLCs. Formulation variables exhibited a significant impact on size, PI and EE of the nanoparticles. SLNs with ∼120 nm size, ∼0.23 PI, ∼I26I mV ZP, ∼87% EE and NLCs with ∼160 nm size, 0.15 PI, ∼I26I mV ZP, ∼88% EE were produced. Cryo-SEM revealed spherical particles with a smooth surface but did not exhibit any difference in surface morphology between SLNs and NLCs. DSC and XRD results demonstrated the disappearance of clotrimazole peak(s) in drug-loaded SLNs and NLCs. Faster drug release was observed from SLNs than NLCs. NLCs were found to be more stable than SLNs in terms of size, PI, EE and drug release. The results indicated that both SLNs and NLCs stabilized with sucrose ester D-1216 can be used as controlled release carriers although NLCs have an edge over SLNs.

The study aims to explore the potential of solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) in improving the topical delivery of capsaicin (CAP) by in vitro and in vivo studies. The lipidic nanoparticles were prepared by solvent diffusion method and were characterized for average particle size, zeta potential and entrapment efficiency. TEM photomicrographs revealed that the particles were nanometric in size. Higher amount of CAP can be encapsulated in the NLCs (87.4 ± 3.28) as compared with SLNs (79.7 ± 2.93%). The cumulative amounts of CAP permeated through the skin and retained in the SC were higher in the case of NLCs as compared with plain drug solution and SLNs. SLNs and NLCs exhibited minimum to no irritation. All the results concluded that NLCs and SLNs have shown a good ability to increase drug accumulation in the various skin layers but NLCs may be a more potential carrier for topical delivery of CAP for an effective therapy of psoriasis.

Objective This review aims to explore innovative therapeutic strategies, with a particular focus on recent advancements in drug delivery systems using bioinspired nanomaterials such as solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) for the idiopathic pulmonary fibrosis (IPF). Significance of the review Current treatments for IPF, including the FDA-approved anti-fibrotic agents pirfenidone and nintedanib, primarily aim to slow disease progression rather than reverse fibrosis. Bioinspired nanomaterials like SLNs and NLCs have shown promise in enhancing the efficacy of anti-fibrotic agents by improving drug solubility, stability, and targeted delivery. These systems not only minimize systemic side effects but also maximize therapeutic impact in lung tissues, offering a new hope for improved patient management and outcomes in this debilitating disease. Key findings SLNs facilitate sustained drug release and have demonstrated potential in delivering phosphodiesterase type 5 inhibitors effectively to lung cells. NLCs, on the other hand, exhibit superior biocompatibility and controlled release properties, making them suitable for pulmonary applications. Studies indicate that both SLNs and NLCs can enhance the bioavailability of drugs like ciprofloxacin and montelukast, thereby improving treatment outcomes in pulmonary conditions. Conclusion The integration of nanotechnology into anti-fibrotic therapy represents a significant advancement in addressing the challenges posed by IPF. By leveraging the unique properties of SLNs and NLCs, there is potential to overcome the limitations of current treatments and provide new therapeutic options that offer better management and improved outcomes for patients suffering from this debilitating disease.

Cancer continues to be one of the leading causes of death worldwide, with 10 million fatalities and 19.3 million new cases reported in 2020. Multidrug resistance (MDR), a formidable issue in chemotherapy, is characterized by the ability of cancer cells to evade cytotoxic drugs through mechanisms such as altered drug targets, disrupted DNA repair, and overexpression of ATP-binding cassette (ABC) transporters like P-glycoprotein (P-gp, responsible for drug efflux). While older oral chemotherapeutics, including 5-fluorouracil (5-FU) and methotrexate, have been effective in certain cancers, their clinical applications are frequently limited by poor bioavailability, dose-limiting toxicities, and drug efflux associated with MDR. Recent evidence supports that incorporating old chemotherapeutic agents into nanocarrier systems such as solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), and mesoporous silica nanoparticles can help overcome key barriers like low solubility, rapid metabolism, and P-gp–mediated efflux. Importantly, the co-delivery of these anti-mitotic drugs alongwith phytochemicals such as curcumin, resveratrol, and astragaloside IV can downregulate drug-efflux transporters, reverse both intrinsic and acquired resistance and increase the efficacy of the chemotherapeutic agents. Among the nanocarrier systems, Lipid-based nanocarriers have demonstrated especial potential in overcoming MDR, including through codelivery. SLNs, for example, have been found to protect drugs from gastrointestinal degradation, facilitate controlled release, and improve oral absorption through lymphatic transport. NLCs, with their “imperfect” lipid matrix, permit higher drug loading and offer superior stability. These platforms have been successfully utilized to boost the bioavailability of agents such as doxorubicin, paclitaxel, and zerumbone. Polymeric micelles, liposomes, and dendrimers have been utilized to co-encapsulate both hydrophilic and hydrophobic compounds, providing additional versatility. This strategy of co-delivery using nanocarriers can be effective not just in disrupting efflux mechanisms and prolonging circulation time, but can also facilitate selective targeting of cancer cells by surface modification using ligands. This integrative approach holds significant potential to rejuvenate conventional drugs, and can make cancer treatment more convenient, potent, and patient-friendly. Keywords : Oral chemotherapy, Multidrug resistance (MDR), Phytochemicals, Nanoparticle co-delivery, potentiating older drugs.

The aim of this study is to evaluate the effect of liquid-to-solid lipid ratio on properties of flurbiprofen-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs), and to clarify the superiority of NLCs over SLNs for transdermal administration. Particle size, zeta potential, drug encapsulation efficiency, in vitro occlusion factor, differential scanning calorimetry, X-ray diffractometry, in vitro percutaneous permeation profile, and stability of SLNs and NLCs were compared. Particle size, zeta potential, drug encapsulation efficiency, in vitro occlusion factor, and in vitro percutaneous permeation amount of the developed NLCs were all <200 nm, < −20 mV, >78%, >35, and >240 μg/cm2, respectively, however, for SLNs were 280 nm, −29.11 mV, 63.2%, 32.54, and 225.9 μg/cm2, respectively. After 3 months storage at 4 °C and 25 °C, almost no significant differences between the evaluated parameters of NLCs were observed. However, for SLNs, particle size was increased to higher than 300 nm (4 °C and 25 °C), drug encapsulation efficiency was decreased to 51.2 (25 °C), in vitro occlusion factor was also decreased to lower than 25 (4 °C and 25 °C), and the cumulative amount was decreased to 148.9 μg/cm2 (25 °C) and 184.4 μg/cm2 (4 °C), respectively. And DSC and XRD studies indicated that not only the crystalline peaks of the encapsulated flurbiprofen disappeared but also obvious difference between samples and bulk Compritol® ATO 888 was seen. It could be concluded that liquid-to-solid lipid ratio has significant impact on the properties of SLNs and NLCs, and NLCs showed better stability than SLNs. Therefore, NLCs might be a better option than SLNs for transdermal administration.

Drug delivery technology has a wide spectrum, which is continuously being upgraded at a stupendous speed. Different fabricated nanoparticles and drugs possessing low solubility and poor pharmacokinetic profiles are the two major substances extensively delivered to target sites. Among the colloidal carriers, nanolipid dispersions (liposomes, deformable liposomes, virosomes, ethosomes, and solid lipid nanoparticles) are ideal delivery systems with the advantages of biodegradation and nontoxicity. Among them, nano-structured lipid carriers and solid lipid nanoparticles (SLNs) are dominant, which can be modified to exhibit various advantages, compared to liposomes and polymeric nanoparticles. Nano-structured lipid carriers and SLNs are non-biotoxic since they are biodegradable. Besides, they are highly stable. Their (nano-structured lipid carriers and SLNs) morphology, structural characteristics, ingredients used for preparation, techniques for their production, and characterization using various methods are discussed in this review. Also, although nano-structured lipid carriers and SLNs are based on lipids and surfactants, the effect of these two matrixes to build excipients is also discussed together with their pharmacological significance with novel theranostic approaches, stability and storage. Solid lipid nanoparticles (SLN) are at the forefront of the rapidly developing field of nanotechnology with several potential applications in drug delivery and research. Due to their unique size dependent properties, lipid nanoparticles offer possibility to develop new therapeutics. The ability to incorporate drugs into nanocarriers offers a new prototype in drug delivery that could use for drug targeting. Hence solid lipid nanoparticles hold great promise for reaching the goal of controlled and site specific drug delivery and hence attracted wide attention of researchers. This review presents a broad treatment of solid lipid nanoparticles discussing their aims, production procedures, advantages, limitations and their possible remedies. Appropriate analytical techniques for the characterization of SLN like photon correlation spectroscopy, scanning electron microscopy, differential scanning calorimetry are highlighted. Aspects of SLN route of administration and the in vivo fate of the carriers are also discussed.

Essential oils are easy to cause oxidative damage, chemical transformation or polymerization, and have some intrinsic problems, such as instability, low water solubility and low bioavailability, which restrict their application in the fields of product development. Nanostructured lipid carriers(NLCs) can overcome some of the restrictions of other colloidal carriers, such as emulsions, liposomes, polymer nanoparticles and solid lipid nanoparticles. NLC is an efficient and stable delivery system for bioactive substances. With unique lipid properties(mixture of solid and liquid lipid), it can overcome the disadvantages of essential oils and protect them from adverse environments, thus improving the stability, bioavailability and safety of essential oils, and achieve sustained release and controlled release. In EOs-NLCs system, essential oils, as special liquid lipid with biological activities and medicinal properties, can fully play the role of medicine-adjuvant integration by changing the structural characteristics of mixed lipid. Based on the development of nanocarriers system, this paper introduces the composition and structural characteristics of EOs-NLCs, and clarifies how to improve the stability of essential oils based on the effects of NLCs on physical and chemical properties, physical stability and release of active components of essential oils. In addition, it also introduces the application of the system in the fields of pharmaceutical, food, cosmetics and skin care products. This review aims to provide some references for improving the stability of essential oils and their applications by using NLCs.

In recent years, herbal nanomedicines have gained tremendous popularity for novel drug discovery. Nanotechnology has provided several advances in the healthcare sector, emerging several novel nanocarriers that potentiate the bioavailability and therapeutic efficacy of the herbal drug. The recent advances in nanotechnology with accelerated strategies of ophthalmic nanosystems have paved a new path for overcoming the limitations associated with ocular drug delivery systems, such as low bioavailability, poor absorption, stability, and precorneal drug loss. Ophthalmic drug delivery is challenging due to anatomical and physiological barriers. Due to the presence of these barriers, the herbal drug entry into the eyes can be affected when administered by following multiple routes, i.e., topical, injectables, or systemic. However, the advancement of nanotechnology with intelligent systems enables the herbal active constituent to successfully entrap within the system, which is usually difficult to reach employing conventional herbal formulations. Herbal-loaded nanocarrier drug delivery systems demonstrated enhanced herbal drug permeation and prolonged herbal drug delivery. In this current manuscript, an extensive search is conducted for original research papers using databases Viz., PubMed, Google Scholar, Science Direct, Web of Science, etc. Further painstaking efforts are made to compile and update the novel herbal nanocarriers such as liposomes, polymeric nanoparticles, solid lipid nanoparticles, nanostructure lipid carriers, micelles, niosomes, nanoemulsions, dendrimers, etc., which are mostly used for ophthalmic drug delivery system. This article presents a comprehensive survey of diverse applications used for the preventative measures and treatment therapy of varied eye disorders. Further, this article highlights the recent findings that the innovators are exclusively working on ophthalmic nanosystems for herbal drug delivery systems. The nanocarriers are promising drug delivery systems that enable an effective and supreme therapeutic potential circumventing the limitations associated with conventional ocular drug delivery systems. The nanotechnology-based approach is useful to encapsulate the herbal bioactive and prevent them from degradation and therefore providing them for controlled and sustained release with enhanced herbal drug permeation. Extensive research is still being carried out in the field of herbal nanotechnology to design an ophthalmic nanosystem with improved biopharmaceutical properties.

Are Nanostructured Lipid Carriers (NLC) better than Solid Lipid Nanoparticles (SLN) for delivering abiraterone acetate through the gastrointestinal tract?

Drug delivery technology has a wide spectrum, which is continuously being upgraded at a stupendous speed. Different fabricated nanoparticles and drugs possessing low solubility and poor pharmacokinetic profiles are the two major substances extensively delivered to target sites. Among the colloidal carriers, nanolipid dispersions (liposomes, deformable liposomes, virosomes, ethosomes, and solid lipid nanoparticles) are ideal delivery systems with the advantages of biodegradation and nontoxicity. Among them, nano-structured lipid carriers and solid lipid nanoparticles (SLNs) are dominant, which can be modified to exhibit various advantages, compared to liposomes and polymeric nanoparticles. Nano-structured lipid carriers and SLNs are non-biotoxic since they are biodegradable. Besides, they are highly stable. Their (nano-structured lipid carriers and SLNs) morphology, structural characteristics, ingredients used for preparation, techniques for their production, and characterization using various methods are discussed in this review. Also, although nano-structured lipid carriers and SLNs are based on lipids and surfactants, the effect of these two matrixes to build excipients is also discussed together with their pharmacological significance with novel theranostic approaches, stability and storage.

Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were prepared as delivery system for water-insoluble anticancer agent, paclitaxel (PTX). The dispersion of SLNs was consisted of 5 % w/w tristearin, 3.75 % w/w egg phosphatidylcholine (egg PC) and 1 % w/w polysorbate 80 in water. NLCs were prepared using the same composition as SLNs except that 10 % of the solid lipid was replaced by triolein. PTX was incorporated into SLNs and NLCs to attain 0.025 % w/w in the dispersion. The particle size of the prepared SLNs and NLCs were 167.9 ± 21.3 and 121.9 ± 28.3 nm, respectively, and slightly increased to 239.1 ± 32.6 and 183.6 ± 36.2 nm by PTX incorporation. PTX incorporation also increased polydispersity index suggesting broader size distribution compared to that for empty particles. SLNs and NLCs showed sustained release of PTX in cell culture media containing 10 % fetal bovine serum at 37 °C compared to the commercial micellar formulation consisted of Cremophor EL and ethanol. PTX in SLNs and NLCs showed comparable cytotoxicity to the commercial formulation and free PTX against human breast cancer cell line, MCF-7. On the contrary, PTX in SLNs and NLCs showed higher anticancer activity against multidrug resistant (MDR) cancer cell line, MCF-7/ADR, compared to the free PTX delivered in DMSO, which indicates that both SLNs and NLCs would be effective carriers to avoid efflux pump expressed in MDR cancer cells. In conclusion, the SLNs and NLCs prepared in the present study showed similar characteristics each other and both can be used as effective delivery system for PTX.

Fungal disease is an invasive, serious, and systemic topical infection that affects the mucous membranes, tissues, and skin of humans. Oral medicines, on the other hand, have significant side effects, making topical treatments a viable alternative. Many antifungal medications applied through the skin in various conventional forms (gels or creams) may cause skin redness, erythema, stinging, and burning sensations. A promising approach to overcome the limitation of conventional form is the use of Nanocarriers for the treatment of skin infections since it allows targeted drug delivery, enhanced skin permeability, and controlled release and hence offers a lower risk of side effects. During the last few decades, lipid nanoparticles (LNPs) such as solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) have gained a lot of attention. SLNs were designed to overcome the drawbacks of conventional colloidal carriers, such as emulsions, liposomes, and polymeric nanoparticles, by offering benefits such as a good release rate and drug targeting with high physical stability. NLCs are SLNs that have been modified (Second generation SLN) to improve stability and capacity loading. This review discusses the pathophysiology of the fungal diseases, the application of SLN and NLC, its method of preparation, Characterization, and an overview of clinical trials on SLN and NLC for the treatment of fungal infection.

Rheumatoid arthritis (RA) is a long-term inflammatory disease that causes synovial joint inflammation, which causes pain, stiffness, and gradual joint destruction. In addition to having a major effect on quality of life, the illness may result in systemic problems. The goal of current treatment approaches, which include biologics, corticosteroids, disease-modifying antirheumatic medications (DMARDs), and nonsteroidal anti-inflammatory medicines (NSAIDs), is to manage symptoms and halt the course of the disease. These treatments, however, frequently have problems like poor effectiveness, systemic side effects, and exorbitant expenses. Advanced, tailored medication delivery methods like nanocarriers are necessary because managing RA is made more difficult by poor patient adherence and limited targeting of inflammatory areas. Berberine and curcumin are bioactive natural compounds with significant therapeutic potential, particularly in managing inflammatory and autoimmune conditions like rheumatoid arthritis (RA). Berberine exhibits potent anti-inflammatory, immunomodulatory, and antioxidant properties, effectively suppressing pro-inflammatory cytokines and oxidative stress Curcumin, a polyphenol derived from turmeric, also demonstrates strong anti-inflammatory and antioxidant effects, inhibiting key molecular pathways involved in RA pathogenesis, such as NF-κB activation. Despite their promising pharmacological profiles, both compounds face challenges like poor water solubility, low bioavailability, and rapid metabolism. Advanced drug delivery systems, such as nanostructured lipid carriers, offer a solution to enhance their therapeutic efficacy and clinical applicability. Nanostructured lipid carriers (NLCs) are advanced drug delivery systems offering numerous advantages for therapeutic applications. Their unique structure, combining solid and liquid lipids, enhances drug solubility, stability, and bioavailability. NLCs enable controlled and sustained drug release, reducing dosing frequency and improving patient compliance. They can protect sensitive drugs like berberine and curcumin from degradation, extending their shelf life. Additionally, NLCs can be functionalized for targeted delivery, increasing drug accumulation at inflamed joints in conditions like rheumatoid arthritis while minimizing systemic side effects. Their biocompatibility and scalability make NLCs a promising platform for improving the clinical efficacy of challenging therapeutic agents. Berberine and curcumin exhibit remarkable anti-inflammatory and antioxidant properties, making them promising candidates for managing rheumatoid arthritis (RA). However, their clinical potential is limited by poor solubility and bioavailability. Nanostructured lipid carriers (NLCs) address these limitations by enhancing drug stability, targeted delivery, and controlled release. Preclinical studies demonstrate improved therapeutic efficacy of NLC formulations in RA models, though clinical translation remains limited. Future research should focus on optimizing NLC designs for enhanced targeting, scalability, and regulatory compliance. Combining these carriers with advanced therapeutic strategies offers a pathway to more effective and patient-friendly RA treatments, bridging lab discoveries to clinical practice