Nanostructured Lipid Carriers Research Articles

Advances in Nanocarrier Systems for Overcoming Formulation Challenges of Curcumin: Current Insights

Curcumin, an organic phenolic molecule that is extracted from the rhizomes of Curcuma longa Linn, has undergone extensive evaluation for its diverse biological activities in both animals and humans. Despite its favorable characteristics, curcumin encounters various formulation challenges and stability issues that can be effectively addressed through the application of nanotechnology. Nano-based techniques specifically focused on enhancing solubility, bioavailability, and therapeutic efficacy while mitigating toxicity, have been explored for curcumin. This review systematically presents information on the improvement of curcumin’s beneficial properties when incorporated, either individually or in conjunction with other drugs, into diverse nanosystems such as liposomes, nanoemulsions, polymeric micelles, dendrimers, polymeric nanoparticles, solid-lipid nanoparticles, and nanostructured lipid carriers. Additionally, the review examines ongoing clinical trials and recently granted patents, offering a thorough overview of the dynamic landscape in curcumin delivery. Researchers are currently exploring nanocarriers with crucial features such as surface modification, substantial loading capacity, biodegradability, compatibility, and autonomous targeting specificity and selectivity. Nevertheless, the utilization of nanocarriers for curcumin delivery is still in its initial phases, with regulatory approval pending and persistent safety concerns surrounding their use.

Optimizing clozapine-loaded nanostructured lipid carriers through central composite design for enhance bioavailability in antipsychotic therapy

Clozapine (CLZ), a tricyclic dibenzodiazepine antipsychotic drug employed for the treatment of Schizophrenia. However, CLZ's significant first-pass effect, poor water solubility, and low oral bioavailability (27%) limit its potential for therapeutic use. The present investigation aimed to prepare CLZ-loaded nanostructured lipid carriers (NLCs) to improve its solubility, bioavailability, and therapeutic efficacy. The NLCs were prepared using an ultrasonic probe sonication technique using selected solid lipids (Gelucire 44/14), liquid lipids (Labrafil M 1944), and surfactants (Monoemul 80). A central composite design approach was adopted to optimize the NLCs. The optimized CLZ-loaded NLCs were evaluated in terms of particle size, zeta potential, surface morphology, crystallinity, drug loading, and in-vitro CLZ release studies. The optimized CLZ-loaded NLCs showed a particle size, zeta potential, and entrapment efficiency of 115.1 ± 2.48 nm, −17 mV and 96.74 ±1.82%, respectively. The morphology revealed the coarsely spherical shape of NLCs. Fourier transform infrared spectroscopy indicated the physical interaction between the CLZ and lipids rather than chemical interaction. The results of powder X-ray diffraction and differential scanning calorimetry showed the conversion of crystalline to amorphous form of CLZ and distributed molecular level in lipid matrix. In the in-vitro release study, pure CLZ showed 14±1.86% release, whereas CLZ-loaded NLC showed initial burst release (20.0±0.56%) followed by sustained release (69.0±1.03%) up to 24 hours. Collectively, results revealed that the developed novel CLZ-loaded NLCs could be a potential formulation to improve efficacy by increasing solubility and prolonging CLZ release and bioavailability with enhanced patient compliance and reduced side effects.

Optimizing Neuroprotective Nano-structured Lipid Carriers for Transdermal Delivery through Artificial Neural Network.

Dementia associated with Alzheimer's disease (AD) is a neurological disorder. AD is a progressive neurodegenerative condition that predominantly impacts the elderly population, although it can also manifest in younger people through the impairment of cognitive functions, such as memory, cognition, and behaviour. Donepezil HCl and Memantine HCl are encapsulated in Nanostructured Lipid Carriers (NLCs) to prolong systemic circulation and minimize the systemic side effects. This work explores the use of data mining tools to optimize the formulation of NLCs comprising of Donepezil HCl and Memantine HCl for transdermal drug delivery. Neuroprotective drugs and excipients are utilized for protecting the nervous system against damage or degeneration. The NLCs were formulated using a high-speed homogenization technique followed by ultrasonication. NLCs were optimized using Box Behnken Design (BBD) in Design Expert Software and artificial neural network (ANN) in IBM SPSS statistics. The independent variables included the ratio of solid lipid to liquid lipid, the percentage of surfactant, and the revolutions per minute (RPM) of the high-speed homogenizer. The NLCs that were formulated had a mean particle size ranging from 67.0±0.45 to 142.4±0.52nm. Both drugs have a %EE range over 75%, and Zeta potential was determined to be - 26±0.36mV. CryoSEM was used to do the structural study. The permeation study showed the prolonged release of the formulation. The results indicate that NLCs have the potential to be a carrier for transporting medications to deeper layers of the skin and reaching systemic circulation, making them a suitable formulation for the management of Dementia. Both ANN and BBD techniques are effective tools for systematically developing and optimizing NLC formulation.

Applicability of QbD-assisted Analytical Method for Simultaneous Detection of Tetrahydrocurcumin and Folic Acid in Developed Nanostructured

Aims:: Applicability of QbD-assisted analytical method for simultaneous detection of tetrahydrocurcumin and folic acid in developed nanostructured. background: Background: Diabetic foot ulcer (DFU), a multifactorial disorder involves chronic inflammation, oxidative stress and neuropathy. Current treatment therapies, involving the use of growth factors and skin substitutes being costly, are out of reach for the majority of patients. The present research explored the usefulness of (5929IN008, application number 202211045937) a combination of tetrahydrocurcumin and folic acid loaded nanostructured lipidic carriers. Background:: Diabetic foot ulcer (DFU) is a multifactorial disorder that involves chronic inflammation, oxidative stress and neuropathy. Current treatment therapies involving the use of growth factors and skin substitutes being costly, are out of reach for the majority of patients. The present research explored the usefulness of (5929IN008, application number 202211045937), a combination of tetrahydrocurcumin and folic acid-loaded nanostructured lipidic carriers. Objectives:: To develop and validate a QbD-assisted method for simultaneous analysis of tetrahydrocurcumin (THC) and folic acid (FA). Applicability of the above method to determine total drug content (TDC) and entrapment efficiency (EE) of nanostructured lipid carriers (NLCs) loaded THC and FA. Methods:: A high-performance liquid chromatographic (HPLC) method was developed, optimized and validated using Box-Behnken design for improved method performance. Chromatographic separation was conducted on a Supelco 250 x 4.6 mm (5 μm) column with optimized mobile phase composition containing tetrahydrofuran: citric acid buffer pH 3.5 (50:50) at a flow rate of 0.4 mL.min-1 and diode array detection between 210 and 360 nm. Results:: The method developed in a concentration range of 1 to 100 μg.mL-1 was found to be linear (R2 0.999, p≤0.001), accurate (99.10-101.70%) and precise with high recovery values in intra and inter-day results. The system adaptability and robustness evaluation revealed that the percent recovery ranged from 96.90 to 102.80%, and the percent relative standard deviation (%RSD) values were less than 2%. Moreover, the method was further applied for the determination of TDC (86±6% and 96±8%) and drug EE (81±21% and 73±13%) for THC and FA, respectively. Conclusion:: The investigation indicated the applicability of the developed and validated method for the estimation of THC and FA in the developed nanostructured lipidic carriers.

Hibiscus sabdariffa-loaded nanostructured lipid carriers (NLC) for fortified nutraceutical milks

Hibiscus sabdariffa-loaded nanostructured lipid carriers (NLC) for fortified nutraceutical milks

Pharmacokinetics and Pharmacodynamics of a Nanostructured Lipid Carrier Co-Encapsulating Artemether and miRNA for Mitigating Cerebral Malaria

Cerebral malaria (CM), a severe neurological pathology caused by Plasmodium falciparum infection, poses a significant global health threat and has a high mortality rate. Conventional therapeutics cannot cross the blood–brain barrier (BBB) efficiently. Therefore, finding effective treatments remains challenging. The novelty of the treatment proposed in this study lies in the feasibility of intranasal (IN) delivery of the nanostructured lipid carrier system (NLC) combining microRNA (miRNA) and artemether (ARM) to enhance bioavailability and brain targeting. The rational use of NLCs and RNA-targeted therapeutics could revolutionize the treatment strategies for CM management. This study can potentially address the challenges in treating CM, allowing drugs to pass through the BBB. The NLC formulation was developed by a hot-melt homogenization process utilizing 3% (w/w) precirol and 1.5% (w/v) labrasol, resulting in particles with a size of 94.39 nm. This indicates an effective delivery to the brain via IN administration. The results further suggest the effective intracellular delivery of encapsulated miRNAs in the NLCs. Investigations with an experimental cerebral malaria mouse model showed a reduction in parasitaemia, preservation of BBB integrity, and reduced cerebral haemorrhages with the ARM+ miRNA-NLC treatment. Additionally, molecular discoveries revealed that nicotinamide adenine dinucleotide phosphate oxidase 2 (NOX2) and Interleukin-6 (IL-6) levels were reduced in the treated groups in comparison to the CM group. These results support the use of nanocarriers for IN administration, offering a viable method for mitigating CM through the increased bioavailability of therapeutics. Our findings have far-reaching implications for future research and personalized therapy.

Lawsone and Lavender Oil Incorporated Nanostructured Lipid Carriers: A Sustained Delivery Platform for Full-Thickness Wound Healing

Lawsone and Lavender Oil Incorporated Nanostructured Lipid Carriers: A Sustained Delivery Platform for Full-Thickness Wound Healing

Nanostructured lipid carrier loaded with Zingiber officinale oil to enhance transdermal bioactive delivery for topical formulation

This study reported on the enhancement of Zingiber officinale (Z. officinale) oil delivery, a bioactive with poor water solubility, by incorporating it into nanostructured lipid carriers (NLC) for transdermal bioactive delivery in topical formulations using the ultrasonication technique with a D–optimal mixture design approach. The independent factors in the process included the percentage of Z. officinale oil, solid lipid (glyceryl monostearate (GMS)), and liquid lipid (virgin coconut oil (VCO)). The study characterized the NLC– Z. officinale oil formulation based on particle size (PS), polydispersity index (PDI), zeta potential (ZP), and encapsulation efficiency (EE) as the dependent variables. Besides, Transmission Electron Microscopy (TEM), Fourier Transform Infrared Spectroscopy with Attenuated Total Reflection (FTIR–ATR), and Differential Scanning Calorimetry (DSC) were also employed. The optimized NLC–Z. officinale oil formulation, comprising 0.36 % Z. officinale oil, 0.14 % solid lipid (GMS), and 0.50 % liquid lipid (VCO). The study's results demonstrated that the finely tuned NLC– Z. officinale oil formulation, with an average diameter of 90.71 ± 9.48 nm, a PDI of 0.147 ± 0.01, a ZP of –45.7 ± 0.67 mV, and an EE of 88.80 ± 11.18 %, exhibited a controlled and sustained release profile following the Korsmeyer–Peppas model. The in vitro penetration studies on excised Sprague–Dawley rat skin and Strat–M® showcased the heightened penetration flux of NLC–Z. officinale oil compared to Z. officinale oil. Furthermore, in vivo distribution studies in female Sprague–Dawley rats underscored the deep penetration of NLCs into the dermal layer after 12 h of application. Notably, a 3–hour treatment with NLC–Z. officinale oil triggered the release of free fatty acids (FFA). The 90 days storage stability study revealed no significant changes in NLC– Z. officinale oil concerning PS and PDI, affirming its stability over time. These findings illuminated the potential applications of NLC– Z. officinale oil as a robust transdermal bioactive delivery system for Z. officinale oil. This underscored its significance in pharmaceutical formulations, providing a novel avenue for therapeutic purposes.

Vitamin D loaded into lipid nanoparticles shows insulinotropic effect in INS-1E cells

Increasing evidence suggests a beneficial role of vitamin D (VitD) supplementation in addressing the widespread VitD deficiency, but currently used VitD3 formulations present low bioavailability and toxicity constrains. Hence, poly(L-lactide-co-glycolide) (PLGA) nanoparticles (NPs), solid-lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were investigated to circumvent these issues. PLGA NPs prepared by emulsification or nanoprecipitation presented 74 or 200 nm, and association efficiency (AE) of 68 % and 17 %, respectively, and a rapid burst release of VitD3. Both SLN and NLCs presented higher polydispersity and larger NPs size, around 500 nm, which could be reduced to around 200 nm by use of hot high-pressure homogenization in the case of NLCs. VitD3 was efficiently loaded in both SLNs and NLCs with an AE of 82 and 99 %, respectively. While SLNs showed burst release, NLCs allowed a sustained release of VitD3 for nearly one month. Furthermore, NLCs showed high stability with maintenance of VitD3 loading for up to one month at 4 °C and no cytotoxic effects on INS-1E cells up to 72 h. A trending increase (around 30 %) on glucose-dependent insulin secretion was observed by INS-1E cells pre-treated with VitD3. This effect was consistently observed in the free form and after loading on NLCs. Overall, this work contributed to further elucidation on a suitable delivery system for VitD3 and on the effects of this metabolite on β cell function.

Emphasis on Nanostructured Lipid Carriers in the Ocular Delivery of Antibiotics.

Drug distribution to the eye is still tricky because of the eye's intricate structure. Systemic delivery, as opposed to more traditional methods like eye drops and ointments, is more effective but higher doses can be harmful. Objective- The use of solid lipid nanoparticles (SLNPs) as a method of drug delivery has been the subject of research since the 1990s. Since SLNPs are derived from naturally occurring lipids, they pose no health risks to the user. To raise the eye's absorption of hydrophilic and lipophilic drugs, SLNs can promote corneal absorption and improve the ocular bioavailability of SLNPs. Methods- To address problems related to ocular drug delivery, many forms of Nano formulation were developed. Some of the methods developed are, emulsification and ultra-sonication, High-speed stirring and ultra-sonication, Thin layer hydration, Adapted melt-emulsification, and ultrasonication techniques, hot o/w micro-emulsion techniques, etc. Results- Nanostructured lipid carriers are described in this review in terms of their ocular penetration mechanism, structural characteristic, manufacturing process, characterization, and advantages over other nanocarriers. Conclusion - Recent developments in ocular formulations with nanostructured bases, such as surface-modified attempts have been made to increase ocular bioavailability in both the anterior and posterior chambers by incorporating cationic chemicals into a wide variety of polymeric systems.

Revolutionizing Wound Healing: Unleashing Nanostructured Lipid Carriers Embodied with Herbal Medicinal Plant.

Wound healing is crucial for maintaining skin integrity and preventing complications from external threats. Various plants, such as Achillea millefolium, Aloe vera, Curcuma longa, Calendula officinalis, Camellia sinensis, Azadirachta indica, and Plantago, have demonstrated wound healing capabilities and have been used in herbal medicine for wound care. NLCs are second-generation lipid nanoparticles, blending solid and liquid lipids to improve medication loading and limit leakage. NLCs have been used in various applications, including cosmeceuticals, chemotherapy, gene therapy, and brain targeting. Wound healing is divided into four stages: hemostasis, inflammatory response, proliferation, and remodeling. Factors such as age, gender, chronic disorders, and local agents like infections can affect recovery. These plants' antiinflammatory, antioxidant, and antibacterial activities have demonstrated potential in wound healing. Combining herbal medicinal plants and nanostructured lipid carriers (NLCs) can revolutionise wound treatment and improve overall healthcare outcomes.

Lesson from nature: Zataria multiflora nanostructured lipid carrier topical gel formulation against Candida-associated onychomycosis, a randomized double-blind placebo-controlled clinical trial

PurposeThe increasing resistance to onychomycosis treatment globally is a major concern as it results in treatment failures. This research aimed to investigate the effectiveness of incorporating nanostructured lipid carriers (NLCs) in a gel formulation for treating mild to moderate Candida-associated onychomycosis using Zataria multiflora (Zt) essential oils. MethodsThe characteristics of Zataria multiflora-loaded nanostructured lipid carriers (Zt-NLCs) were validated using a carbopol gel (1 % w/w). In vitro tests were conducted using CLSI M60 standards to evaluate the susceptibility of ten commonly encountered dermatophyte species to antifungal agents. A clinical study was conducted involving 40 volunteers randomly assigned to two groups: one receiving the Zt-NLCs gel and the other receiving a placebo, using a double-blind, placebo-controlled design. The objective was to assess clinical manifestations and mycological findings after topical application for 2 and 4 weeks. The causative agents' species were identified using a PCR-RFLP method. ResultsThe preparation of Zt-NLCs gel resulted in a uniform suspension of spherical nanoparticles with favourable characteristics and no cytotoxic effects. Zt-NLCs demonstrated significant inhibitory effects on fungal growth and effectively improved clinical and mycological criteria in comparison to the placebo group (p < 0.005), even after 2 weeks of treatment. The C. albicans complex was recognized as the predominant species isolated from the patients using PCR-RFLP. ConclusionThe administration of Zt-NLCs gel for two weeks showed significant efficacy in disease management, as reported by both dermatologists and mycologists and therefore shows its potential use as a treatment against Candidal onychomycosis.

Physical characterization and bioavailability assessment of 5-fluorouracil-based nanostructured lipid carrier (NLC): In vitro drug release, Hemolysis, and permeability modulation.

5-Fluorouracil (5-FU) is an anticancer agent belonging to BCS Class III that exhibits poor release characteristics and low retention in the biological system. The main objective of this investigation was to develop a drug delivery system, i.e., Nanostructure Lipid Carriers (NLCs) loaded with 5-FU to prolong its biological retention through 5-FU-loaded NLCs (5-FUNLC) were designed to manipulate physicochemical characteristics and assessment of in vitroandin vivoperformance. The developed NLCs underwent comprehensive characterization, including assessments for particle size, zeta potential, morphological evaluation, and FT-IR spectroscopy. Additionally, specific evaluations were conducted for 5-FUNLCs, encompassing analyses for encapsulation efficiency of the drug, release characteristics in PBS at pH 6.8, and stability study. The lipophilic character of 5-FUNLC was confirmed through the measurement of the partition coefficient (log P). 5-FUNLCs were observed as spherical-shaped particles with a mean size of 300 ± 25nm. The encapsulation efficiency was determined to be 89%, indicating effective drug loading within the NLCs. Furthermore, these NLCs exhibited a sustained release nature lasting up to 3-4h, indicating their potential for controlled drug release over time. Lipid components were biocompatible with the 5-FU to determine thermal transition temperature and show good stability for 30days. Additionally,an in vitrohemolysis study that confirmed the system did not cause any destruction to the RBCs during intravenous administration. The drug's gut permeability was assessed utilizing the optimized 5-FUNLC (F2) in comparison to 5-FU through the intestine or gut sac model (in the apical to basolateral direction, A → B). The permeability coefficient was measured as 4.91 × 10-5cm/h with a significant difference. Additionally, the antioxidant potential of the NLCs was demonstrated through the DPPH method. The NLCs' performance was further assessed throughin vivopharmacokinetic studies on Wistar Rats, resulting in a 1.5-fold enhancement in their activity compared to free 5-FU. These NLCs offer improved drug solubility and sustained release, which collectively contribute to enhanced therapeutic outcomes and modulate bioavailability. The study concludes by highlighting the potential of 5-FUNLC as an innovative and efficient drug delivery system. The findings suggest that further preclinical investigations are warranted, indicating a promising avenue for the development of more effective and well-tolerated treatments for cancer.

Ibrutinib topical delivery for melanoma treatment: The effect of nanostructured lipid carriers’ composition on the controlled drug skin deposition

Melanoma is responsible for more than 80% of deaths related to skin diseases. Ibrutinib (IBR), a Bruton's tyrosine kinase inhibitor, has been proposed to treat this type of tumor. However, its low solubility, extensive first-pass effect, and severe adverse reactions with systemic administration affect therapeutic success. This study proposes developing and comparing the performance of two compositions of nanostructured lipid carriers (NLCs) to load IBR for the topical management of melanomas in their early stages. Initially, the effectiveness of IBR on melanoma proliferation was evaluated in vitro, and the results confirmed that the drug reduces the viability of human melanoma cells by inducing apoptosis at a dose that does not compromise dermal cells. Preformulation tests were then conducted to characterize the physical compatibility between the drug and the selected components used in NLCs preparation. Sequentially, two lipid compositions were used to develop the NLCs. Formulations were then characterized and subjected to in vitro release and permeation tests on porcine skin. The NLCs containing oleic acid effectively controlled IBR release over 24 h compared to the NLCs composed of pomegranate seed oil. Furthermore, the nanoparticles acted as permeation enhancers, increasing the fluidity of the lipids in the stratum corneum, as determined by EPR spectroscopy, which stimulated the IBR penetration more profoundly into the skin. However, the NLCs composition also influenced the permeation promotion factor. Thus, these findings emphasize the importance of the composition of NLCs in controlling and increasing the skin penetration of IBR and pave the way for future advances in melanoma therapy.

Validation of spectrophotometric methods for the simultaneous determination of fluconazole and riparin B in the development of lipid nanoparticles modified by β-cyclodextrin: Application for in vitro characterization and ex vivo studies of nail retention

Fluconazole (FLC) has been used in the clinic for almost thirty years as a treatment for fungal infections, but its widespread use has led to the emergence of resistant strains. In this context, synthetic analogues of riparins, phytocompounds isolated from Aniba riparia (Nees) Mez (Lauraceae), such as Riparin B (RIP), stand out as an important agent for modulating antimicrobial resistance, potentially useful for treating superficial mycoses resistant to conventional antifungals. Onychomycosis is one of the main fungal infections affecting the nails. Its local treatment is desirable but has limited efficacy due to poor drug permeation. The use of nanoparticles and permeation promoters can increase permeability and improve treatment. Therefore, nanostructured lipid carriers coated with β-cyclodextrin (MNLC) were developed for the topical application of FLC and RIP on nails. To support the formulation, four spectrophotometric methods (amplitude factor, amplitude subtraction, modified amplitude subtraction, and fourth-order derivative), based on derivative spectroscopy and simple mathematical manipulations, were validated, in accordance with the International Conference on Harmonization (ICH), for simultaneous determination of FLC and RIP in the MNLC and in in vitro characterization studies of the formulation. In addition, the methods were applied to quantify drug retention in porcine hooves using an optimized extraction process. All the methods developed were found to be linear (r > 0.999), precise (RSD < 5 %), and accurate (92.33 to 108.86 %) without being affected by the components of the formulation or the biological matrix. The methods developed made it possible to determine the encapsulation efficiency and sustained release profile of the drugs. In addition, successive extractions revealed the amount of FLC and RIP retained in the superficial and deeper regions of porcine hooves. Thus, the results indicated that FLC and RIP can be determined simultaneously, quickly, simply, and economically, using any of the proposed methods, in complex MNLC samples and the biological matrix of porcine hooves.

NLC-Based Sunscreen Formulations with Optimized Proportion of Encapsulated and Free Filters Exhibit Enhanced UVA and UVB Photoprotection.

The topical use of sunscreens is recommended for avoiding the damaging effects of UV radiation. However, improvements are still needed in the existing products to enhance their photoprotection effectiveness and safety. This involves minimizing the use of chemical UV filters while providing enhanced and prolonged photoprotection. This work investigated novel sunscreen formulations and their UV protection effects by encapsulating Uvinul® A, Tinosorb® S, and Uvinul® T150 into nanostructured lipid carriers (NLCs) based on bacuri butter and raspberry seed oil. First, the impact of critical formulation and process parameters on NLCs' particle size was evaluated using a 22 Face Centered Central Composite Design. Then, formulations were evaluated in terms of critical quality factors, in vitro skin permeation, and in vitro and in vivo photoprotection activities. The developed NLCs-containing formulations exhibited appropriate size (122-135 nm), PdI (<0.3), encapsulation efficiency (>90%), and drug content (>80%), which were preserved for at least 90 days under different stability conditions. Moreover, these NLCs-based formulations had equivalent skin permeation to emulsion-based controls, and the addition of NLCs into sunscreen cream bases in the optimum proportion of 20% (w/w) resulted in enhanced UVA and UVB photoprotection levels, despite a 10% reduction in the total filters content. Altogether, these results describe the application of nanoencapsulated organic UV filters in innovative sunscreen formulations to achieve superior photoprotection and cosmeceutical properties.

Recent Advances in Development of Vesicular Carrier for Transdermal Drug Delivery: A Review

Transdermal drug delivery has gained significant attention as a non-invasive and convenient method for administering drugs. However, the stratum corneum, the outermost layer of the skin, poses a significant barrier to drug permeation. To overcome this challenge, vesicular carriers have emerged as promising systems for enhancing drug delivery through the skin. This review highlights recent advances in the development of vesicular carriers for transdermal drug delivery. Liposomes, niosomes, transfersomes, ethosomes, and solid lipid nanoparticles are among the commonly used vesicular carriers. These carriers offer advantages such as improved drug solubility, prolonged drug release, and enhanced drug stability. Additionally, they can encapsulate a wide range of drugs, including hydrophilic and lipophilic compounds. Various strategies have been employed to optimize vesicular carriers for transdermal drug delivery. These include modifying the vesicle composition, size, and surface charge to enhance skin penetration. The incorporation of penetration enhancers, such as surfactants, has also been explored to improve drug permeation across the skin. Furthermore, advancements in nanotechnology have led to the development of novel vesicular carriers, such as nanostructured lipid carriers and elastic liposomes. These carriers offer improved drug loading capacity, sustained release profiles, and enhanced skin penetration. Moreover, the use of vesicular carriers has shown promise in delivering a wide range of therapeutic agents, including small molecules, peptides, proteins, and genetic material. The ability to encapsulate and deliver these diverse drug entities opens new possibilities for transdermal drug delivery in various therapeutic areas.

Natural Stabilizers and Nanostructured Lipid Carrier Entrapment for Photosensitive Compounds, Curcumin and Capsaicin.

Capsaicin and curcumin, the active components of chili and turmeric, are prone to instability when exposed to light. Therefore, this research aimed to enhance the photostability of both extracts via the use of antioxidants, natural sunscreen, and nanostructured lipid carriers (NLCs). NLCs were chosen for this this study due to their advantages in terms of stability, drug loading capacity, occlusive effect, skin penetration, and controlled release. The photostability of each extract and extracts mixed with antioxidants, including grape seed extract, tea extract, and chlorogenic acid, were determined. Chlorogenic acid can enhance the photostability of capsaicin from 6.79 h to 16.50 h, while the photostability of curcumin increased from 9.63 h to 19.25 h. In addition, the use of natural sunscreen (sunflower oil) also increased the photostability of capsaicin and curcumin. The mixed extracts were then loaded into NLCs. The particle size of the formulation was 153.73 nm with a PDI value of 0.25. It exhibited high entrapment efficiency (more than 95%). In addition, it effectively reduced the decomposition of capsaicin and curcumin. Importantly, the natural stabilizers chosen for NLC fabrication significantly improved the photostability of curcumin and capsaicin by 600% and 567% compared to the unstabilized counterparts. This improvement contributes to the sustainability and bioavailability of these compounds in both cosmeceutical and pharmaceutical products.

Engineering of smart nanostructured lipid carriers encapsulated in gold nanocomposites and camptothecin for synergistic photothermal and chemotherapy treatment of ovarian cancer

Engineering of smart nanostructured lipid carriers encapsulated in gold nanocomposites and camptothecin for synergistic photothermal and chemotherapy treatment of ovarian cancer

Development and evaluation of hyaluronic acid conjugated tacrolimus-loaded nanostructured lipid carriers using moringa oleifera seed oil as liquid lipid

The proposed research work aims to develop hyaluronic acid conjugated tacrolimus-loaded nanostructured lipid carriers (HYA-TAC-loaded-SA-NLCs) to improve the release rate and cellular uptake to enhance its oral absorption. TAC-loaded-SA-NLCs were prepared using stearylamine as solid lipid and Moringa oleifera (MO) seed oil. The conjugation of hyaluronic acid (HYA) to the surface of TAC-loaded-SA-NLCs was done using electrostatic interaction between stearylamine and HYA. Further, the conjugation is confirmed by using zeta potential and FTIR (Fourier transform infrared) spectroscopy. In-vitro release study showed ∼12 and ∼11 times more drug dissolution efficiency from TAC-loaded-SA-NLCs and HYA-TAC-loaded-SA-NLCs than TAC-suspension. The in-vitro protein denaturation studies showed that HYA-TAC-loaded-SA-NLCs had a lower IC50 than TAC-loaded-SA-NLCs and TAC suspension. Furthermore, the cellular uptake studies in HCT-116 cells showed enhanced cellular uptake of unmodified NLCs (∼2.5 times) and HYA modified NLCs (∼8.4 times) than suspension. The storage stability study revealed no significant change in the lyophilized HYA-TAC-loaded-SA-NLCs after 3 months. Hence, the study concluded that the prepared HYA modified NLCs could significantly improve the cellular uptake and anti-inflammatory activity.