Lipid-based Nanocarriers Research Articles

Nanocarrier-Based Transdermal Drug Delivery Systems for Dermatological Therapy

Dermatoses are among the most prevalent non-fatal conditions worldwide. Given this context, it is imperative to introduce safe and effective dermatological treatments to address the diverse needs and concerns of individuals. Transdermal delivery technology offers a promising alternative compared to traditional administration methods such as oral or injection routes. Therefore, this review focuses on the recent achievements of nanocarrier-based transdermal delivery technology for dermatological therapy, which summarizes diverse delivery strategies to enhance skin penetration using various nanocarriers including vesicular nanocarriers, lipid-based nanocarriers, emulsion-based nanocarriers, and polymeric nanocarrier according to the pathogenesis of common dermatoses. The fundamentals of transdermal delivery including skin physiology structure and routes of penetration are introduced. Moreover, mechanisms to enhance skin penetration due to the utilization of nanocarriers such as skin hydration, system deformability, disruption of the stratum corneum, surface charge, and tunable particle size are outlined as well.

Novel Delivery Systems of Raloxifene Hydrochloride for Improved Bioavailability and Therapeutic Efficacy: A Review

Raloxifene hydrochloride belongs to the selective estrogen receptor modulator category. Initially, US FDA approved its use for the prevention and treatment of osteoporosis in postmenopausal women. Later, raloxifene hydrochloride was also approved for the prevention of invasive breast carcinoma in post-menopausal women under the high-risk category. Despite its immense and diverse therapeutic potential, the oral bioavailability of raloxifene hydrochloride is only ~ 2%. The factors responsible for the poor bioavailability of raloxifene hydrochloride include its amphiphobic nature, para-glycoprotein pump-mediated efflux in the intestine, and high pre-systemic glucuronidation. In the past two decades, multiple novel delivery systems, viz. lipid-based nanocarriers, polymeric nanoparticles, polymer-lipid hybrid nanoparticles, micelles, and mixed micelles, have been developed to overcome its drawbacks. Moreover, inclusion complex, phospholipid complex, and solid dispersion have also been developed to improve its solubility and dissolution rate. Further, some research groups successfully explored non-peroral routes like nasal and transdermal for augmenting the raloxifene hydrochloride bioavailability and its therapeutic efficacy. Hence, the principal objective of this review paper is to critically analyze all the delivery systems developed for raloxifene hydrochloride with their advantages and limitations. In addition, a detailed discussion of the physicochemical and pharmacokinetic parameters of raloxifene hydrochloride has been included in this paper. An in-depth understanding of these parameters will assist formulation scientists in developing efficient delivery systems in the future. In conclusion, the literature review revealed that the nanoparticulate systems successfully augmented the raloxifene hydrochloride bioavailability and therapeutic efficacy in pre-clinical experiments. However, future clinical trials should be conducted to assess their safety and therapeutic efficacy for rapid preclinical to clinical translation.

Lipid-based Non-viral Vector: Promising Approach for Gene Delivery.

The present review aims to discuss various strategies to overcome intracellular and extracellular barriers involved in gene delivery as well as the advantages, challenges, and mechanisms of gene delivery using non-viral vectors. Additionally, patents, clinical studies, and various formulation approaches related to lipid-based carrier systems are discussed. Data were searched and collected from Google Scholar, ScienceDirect, Pubmed, and Springer. In this review, we have investigated the advantages of non-viral vectors over viral vectors. The advantage of using non-viral vectors are that they seek more attention in different fields. They play an important role in delivering the genetic materials. However, few nonviral vector-based carrier systems have been found in clinical settings. Challenges are developing more stable, site-specific gene delivery and conducting thorough safety assessments to minimize the undesired effects. In comparison to viral vectors, nonviral vector-based lipid nanocarriers have more advantages for gene delivery. Gene therapy research shows promise in addressing health concerns. Lipid-based nanocarriers can overcome intracellular and extracellular barriers, allowing efficient delivery of genetic materials. Non-viral vectors are more attractive due to their biocompatibility, ease of synthesis, and cost-effectiveness. They can deliver various nucleic acids and have improved gene delivery efficacy by avoiding degradation steps. Despite limited clinical use, many patents have been filed for mRNA vaccine delivery using non-viral vectors.

Enhancing Nutraceutical Bioavailability with Bilosomes: A Comprehensive Review

Nutraceuticals, encompassing vitamins, minerals, and dietary supplements, play a pivotal role in promoting health and wellness. However, their therapeutic efficacy is often hindered by poor bioavailability. Bilosomes, a burgeoning lipid-based nanocarrier, have emerged as a promising solution to overcome this challenge. This comprehensive review explores the potential of bilosomes as carriers for enhancing the bioavailability of nutraceuticals, shedding light on their formulation, characterization, mechanisms of action, safety considerations, and future prospects. The review begins by delineating the significance of nutraceuticals in promoting well-being and discusses the obstacles associated with their delivery. It subsequently introduces bilosomes, lipid vesicles equipped with bile salts, and elucidates their advantages over traditional delivery systems. A comparative analysis with other lipid-based carriers underscores the unique attributes that make bilosomes an attractive choice for nutraceutical delivery. A deeper dive into bilosome formulation and characterization provides insights into lipid composition, encapsulation techniques, and physicochemical characterization methods. Factors influencing bilosome stability and bioavailability, including size, surface charge, and interactions with physiological barriers, are comprehensively reviewed. Safety and toxicological considerations related to bilosome-based nutraceutical delivery are meticulously examined, drawing from preclinical and clinical studies. Regulatory aspects pertinent to bilosome incorporation in nutraceutical products are outlined. Future perspectives delve into emerging trends, formulation challenges, and the potential for personalized nutrition with bilosomes. In conclusion, this review underscores the transformative potential of bilosomes in enhancing nutraceutical bioavailability, opening new vistas in the field of personalized nutrition and health promotion.

Lipid-based nanodelivery systems of curcumin: Recent advances, approaches, and applications

Despite its many beneficial effects, pharmaceutical applications of curcumin (CUR) are limited due to its chemical instability, low solubility/absorption and weak bioavailability. Recent advances in nanotechnology have enabled the development of CUR-loaded nanodelivery systems to tackle those issues. Within many different nanocarriers developed for CUR up to date, lipid-based nanocarriers (LBNs) are among the most extensively studied systems. LBNs such as nanoemulsions, solid lipid carriers, nanostructured phospholipid/surfactant carriers are shown to be potential delivery systems capable of improving the solubility, bioavailability, and chemical stability of CUR. The particle characteristics, stability, bioavailability, and release properties of CUR-loaded LBNs can be tailored via optimizing the formulation and processing parameters. This paper reviews the most recent studies on the development of various CUR-loaded LBNs. Approaches to the improvement of CUR bioavailability and release characteristics of LBNs are discussed. Furthermore, challenges in the development of CUR-loaded LBNs and their potential applications are presented.

Lipid-Based Nanocarriers: Bridging Diagnosis and Cancer Therapy.

Theranostics is a growing field that matches diagnostics and therapeutics. In this approach, drugs and techniques are uniquely coupled to diagnose and treat medical conditions synergically or sequentially. By integrating diagnostic and treatment functions in a single platform, the aim of theranostics is to improve precision medicine by tailoring treatments based on real-time information. In this context, lipid-based nanocarriers have attracted great scientific attention due to their biodegradability, biocompatibility, and targeting capabilities. The present review highlights the latest research advances in the field of lipid-based nanocarriers for cancer theranostics, exploring several ways of improving in vivo performance and addressing associated challenges. These nanocarriers have significant potential to create new perspectives in the field of nanomedicine and offer promise for a significant step towards more personalized and precise medicine, reducing side effects and improving clinical outcomes for patients. This review also presents the actual barriers to and the possible challenges in the use of nanoparticles in the theranostic field, such as regulatory hurdles, high costs, and technological integration. Addressing these issues through a multidisciplinary and collaborative approach among institutions could be essential for advancing lipid nanocarriers in the theranostic field. Such collaborations can leverage diverse expertise and resources, fostering innovation and overcoming the complex challenges associated with clinical translation. This approach will be crucial for realizing the full potential of lipid-based nanocarriers in precision medicine.

Lipid Nanoparticles for Brain Tumor Theranostics: Challenges and Status.

Lipid nanoparticles have been recognized as a powerful weapon for delivering various imaging and therapeutic agents to the localized solid tumors, especially brain tumors individually or in combination. Promisingly, lipid-based nanosystems have been considered as safe delivery systems which are even approved by the Food and Drug Administration (FDA) and the European Medicines Agency (EMA). One recent spotlight of lipid nanoparticles as COVID-19 mRNA vaccines where lipid nanoparticles play an important role in effectively protecting and delivering mRNA to the desired cells. As of now, successive progress in lipid-based nanocarriers, viz., nanoliposomes, solid lipid nanoparticles, ionizable lipid nanostructures, etc., with better biochemical and biophysical stabilities, has been noticed and reported. Moreover, lipid nanostructures have been considered as versatile therapeutics platforms for a variety of diseases due to their biocompatibility, ability to protect and deliver therapeutics to the localized site, and better reproducibility and reliability. However, lipid nanoparticles still face morphological and biochemical changes upon their in vivo administration. These changes alter the specific biological and pathological response of lipid nanoparticles during their personalized brain tumor theranostics. Second, lipid nanomedicine still faces major challenges of zero premature leakage of loaded cargo, long-term colloidal stability, and off targeting. Herein, various lipid-based nanomedicines for brain tumor imaging and therapeutics "theranostics" have been reviewed and summarized considering major aspects of preclinical and clinical studies. On the other hand, engineering and biological challenges of lipid theranostics systems with relevant advantages and guidelines for clinical practice for different brain tumors have also been discussed. This review provides in-depth knowledge of lipid nanoparticle-based theranostics agents for brain tumor imaging and therapeutics.

PEGylation in Pharmaceutical Development: Current Status and Emerging Trends in Macromolecular and Immunotherapeutic Drugs.

The purpose of the research is to examine the advantages and difficulties of target-site drug delivery methods, with an emphasis on the application of polyethylene glycol (PEG) to enhance drug solubility, bioavailability, and immune response characteristics. It has been demonstrated that this method lowers immunogenicity, enhances pharmacokinetics, and helps drugs pass the blood-brain barrier while reducing reticuloendothelial system clearance. PEG and its derivatives are being used more and more to alter therapeutic substances, offering an escape from some of the drawbacks of conventional medication formulations. In the review, different PEGylation tactics are examined, including cutting-edge methods for reversing multi-drug resistance in nanocarriers. PEGylation has a number of benefits, but there are still drawbacks, including the immunogenic reaction to PEG, which is sometimes referred to as "anti-PEG antibodies," and stability problems that call for the creation of countermeasures. The study devotes a large amount of its space to listing FDA-approved PEGylated medications, emphasizing their therapeutic advantages and clinical uses in a range of medical specialties. The research also explores the regulatory environment that surrounds PEG, closely examining its effectiveness and safety in medication compositions. The review goes beyond PEGylation and includes lipid-based nanocarriers, including liposomes, nanostructured lipid carriers (NLCs), and solid lipid nanoparticles (SLNs). Because these nanocarriers can target specific tissues or cells, improve bioavailability, and encapsulate pharmaceuticals, they are becoming more and more significant in drug delivery systems. The Target Product Profile (TPP) and Quality by Design (QbD) principles serve as the foundation for the creation and characterization of these lipid-based systems. These tools direct the methodical assessment of material properties and risk assessments during the formulation phase. This method guarantees that the finished product satisfies the appropriate requirements for efficacy, safety, and quality. The regulatory status and safety profile of nano lipid carriers are covered in the paper's conclusion, which emphasizes the importance of careful examination and oversight in bringing these cutting-edge products to market. Overall, this thorough analysis highlights the revolutionary potential of lipid-based nanocarriers and PEGylation in improving drug delivery and therapeutic efficacy, but it also draws attention to the continued difficulties and legal issues that need to be resolved in order to fully reap the benefits of these technologies in biomedicine.

Lipid-based nanocarriers mediated Axitinib retinal delivery after topical instillation: Formulations setting up and in vivo evidence

Axitinib (AXB) is a multi-receptor tyrosine kinase inhibitor molecule. It acts by blocking the receptors for vascular endothelial growth factor (VEGFR) and platelet-derived growth factor (PDGFR), which are responsible for the development of neovascularization. To date, intravitreal injections of anti-VEGF have become the first-line medical treatment for diabetic macular oedema, a degeneration of diabetic retinopathy. Despite the efficacy of intravitreal injections, the complications of this type of administration are manifold. Our study aimed to design a nanotechnological formulation capable of delivering AXB to the retinal area after topical administration. Two different lipid-based formulations, namely solid lipid nanoparticles (SLN) and nanostructured lipid nanocarriers (NLC) were developed through a design of experiment (DoE) approach. The formulations possessed a mean particle size below 200 nm, low PDI values and a high drug encapsulation efficiency, thus designating them as suitable for ocular administration. Stability studies were performed at different storage conditions according to ICH guidelines. Strategies to improve AXB concentration in the retinal target were finally developed, such as using cationic lipids and increasing AXB loading in the nanocarriers. The in vivo PK studies indicated that cationic NLC loaded with AXB at 4 mM were the most efficient in delivering the drug to the retina, proposing them as a potential topical treatment for DR.

Virgin Coconut Oil-based Nanostructured Lipid Carrier Improves the Hypolipidemic Effect of Rosuvastatin.

Monitoring noncommunicable diseases is regarded as a critical concern that has to be managed in order to avoid a wide variety of complications such as increasing blood lipid levels known as dyslipidemia. Statin drugs, mostly, Rosuvastatin (RSV) was investigated for its effectiveness in treating dyslipidemia. However, reaching the most efficient treatment is essential and improving the effect of RSV is crucial. Therefore, a combination therapy was a good approach for achieving significant benefit. Although RSV is hydrophobic, which would affect its absorption and bioavailability following oral administration, overcoming this obstacle was important. To that end, the purpose of the present investigation was to incorporate RSV into certain lipid-based nanocarriers, namely, nanostructured lipid carrier (NLC) prepared with virgin coconut oil (CCO). The optimized RSV-NLC formula was selected, characterized and examined for its in vitro, kinetic, and stability profiles. Eventually, the formula was investigated for its in vivo hypolipidemic action. The optimized NLC formulation showed a suitable particle size (279.3±5.03 nm) with PDI 0.237 and displayed good entrapment efficiency (75.6±1.9%). Regarding in vitro release, it was efficiently prolonged for 24 h providing 93.7±1.47%. The optimized formula was established to be stable after 3 months storage at two different conditions; 4°C and 25°C. Importantly, including CCO in the development of RSV-NLC could impressively enhance lowering total cholesterol level in obese rat models, which endorse the potential synergistic action between RSV and CCO. The study could elucidate the impact of developing NLC using CCO for improving RSV anti-hyperlipidemic activity.

Exploring the Therapeutic Potential of Natural Compounds in Psoriasis and Their Inclusion in Nanotechnological Systems.

Psoriasis is a chronic inflammatory disease that affects around 2-3% of the world's population. The treatment for this autoimmune disease still remains centered around conventional methods using synthetic substances, even though more recent advancements focus on biological therapies. Given the numerous side effects of such treatments, current research involves plant extracts and constituents that could prove useful in treating psoriasis. The aim of this narrative review is to highlight the most known representatives belonging to classes of natural compounds such as polyphenols (e.g., astilbin, curcumin, hesperidin, luteolin, proanthocyanidins, and resveratrol), alkaloids (e.g., berberine, capsaicin, and colchicine), coumarins (psoralen and 8-methoxypsoralen), and terpenoids (e.g., celastrol, centelloids, and ursolic acid), along with plants used in traditional medicine that could present therapeutic potential in psoriasis. The paper also provides an overview of these compounds' mechanisms of action and current inclusion in clinical studies, as well as an investigation into their potential incorporation in various nanotechnological systems, such as lipid-based nanocarriers or polymeric nanomaterials, that may optimize their efficacy during treatment.

Enhanced Skin Penetration and Efficacy: First and Second Generation Lipoidal Nanocarriers in Skin Cancer Therapy.

Skin carcinoma remains one of the most widespread forms of cancer, and its global impact continues to increase. Basal cell carcinoma, melanoma, and squamous cell carcinoma are three kinds of cutaneous carcinomas depending upon occurrence and severity. The invasive nature of skin cancer, the limited effectiveness of current therapy techniques, and constraints to efficient systems for drug delivery are difficulties linked with the treatment of skin carcinoma. In the present era, the delivery of drugs has found a new and exciting horizon in the realm of nanotechnology, which presents inventive solutions to the problems posed by traditional therapeutic procedures for skin cancer management. Lipid-based nanocarriers like solid lipid nanoparticles and nanostructured lipid carriers have attracted a substantial focusin recent years owing to their capability to improve the drug'ssite-specific delivery,enhancing systemic availability,and thus its effectiveness. Due to their distinct structural and functional characteristics, these nanocarriers can deliver a range of medications, such as peptides, nucleic acids, and chemotherapeutics, via different biological barriers, such as the skin. In this review, an effort was made to present the mechanism of lipid nanocarrier permeation via cancerous skin. In addition, recent research advances in lipid nanocarriers have also been discussed with the help of in vitro cell lines and preclinical studies. Being a nano size, their limitations and toxicity aspects in living systems have also been elaborated.

Emerging Trends in Targeted Magnetic Nanoparticle Imaging for Precision Medicine in Oncology

In cancer care's dynamic landscape, targeted imaging is pivotal for advancing precision medicine. This review focuses on the role of magnetic nanoparticles (MNPs), particularly magnetic iron oxide nanoparticles (MIONPs) and superparamagnetic iron oxide nanoparticles (SPIONs), in personalized diagnostics and treatments for oncology. Current trends and future directions in MNP imaging, addressing challenges like biocompatibility, toxicity, and regulatory considerations, are discussed. The review explores MIONPs' theranostic potential, especially in brain drug delivery monitoring through magnetic resonance imaging (MRI) or magnetic particle imaging (MPI). Variousnanoparticle types, including SPIONs as MRI contrast agents, are highlighted. The article covers challenges in nanoparticle modification, including methoxy- polyethylene glycol (mPEG), and discusses gold nanoparticles (AuNPs) for photoacoustic imaging, as well as insights into fluorescent semiconductor quantum dots (QDs). The conclusion emphasizes rapid and accurate tumoridentification, introduces carbon nanotubes (CNTs) for cancer therapy and diagnosis, and underscores the transformative role of lipid-based nanocarriers incancer research. The multifaceted applications of nanotechnology in cancer diagnostics and treatment are discussed throughout, showcasing a paradigm shift.Crucial challenges in unlocking nanotechnology's full potential in cancer care, such as safety concerns, robust clinical trials, synthesis methods standardization, regulatory approval, biodegradability, tailoring nanotherapies, economic viability, ethical considerations, and interdisciplinary collaboration, are addressed. Addressing these challenges holds the promise of elevating nanotechnology into a potent force in the ongoing battle against cancer.

Resveratrol-loaded lipid-based nanocarriers for topical delivery: Comparative physical properties and antioxidant activity

Resveratrol (R) is an antioxidant that helps several aspects of aging skin. However, it is slightly soluble in water and unstable under light exposure, necessitating the use of suitable formulations for improved clinical efficacy. Therefore, this study aimed to prepare R-loaded lipid-based nanocarriers for topical delivery, i.e., nanostructured lipid carriers (NLCs) and nanoemulsions (NEs). R-loaded nanocarrier gels were further prepared to increase R loading. The comparative physical properties and antioxidant activity of nanocarriers were performed in terms of particle size, zeta potential, morphology, rheology, R content, in vitro release, antioxidant activity, cytotoxicity and stability. The results revealed that R was successfully loaded into NLCs and NE gels (NEGs), having different physical properties and antioxidant activity depending on the composition of lipid-based nanocarriers. R could be incorporated into NEs and the aqueous gelling phase, resulting in higher R loading. Furthermore, the gelling network was responsible for pseudoplastic flow behavior. The cumulative amount of R released from NEGs was significantly higher than that from NLCs due to the co-surfactant-like properties of NEGs, which resulted in smaller particle sizes. However, NLCs exhibited significantly more antioxidant activity and less cytotoxicity compared to NEGs. The stability of both nanosystems showed no significant change when stored at refrigerator temperature for over 3 months. In conclusion, the various compositions of lipid-based nanocarriers produced a range of physical properties and antioxidant activity. Nonetheless, these NLCs and NEGs have the potential to be nanocarriers for R, which has antioxidant properties for topical application.

Demystifying the potential of lipid-based nanocarriers in targeting brain malignancies.

Drug targeting for brain malignancies is restricted due to the presence of the blood-brain barrier (BBB) and blood-brain tumor barrier (BBTB), which act as barriers between the blood and brain parenchyma. Certainly, the limited therapeutic options for brain malignancies have made notable progress with enhanced biological understanding and innovative approaches, such as targeted therapies and immunotherapies. These advancements significantly contribute to improving patient prognoses and represent a promising shift in the landscape of brain malignancy treatments. A more comprehensive understanding of the histology and pathogenesis of brain malignancies is urgently needed. Continued research focused on unraveling the intricacies of brain malignancy biology holds the key to developing innovative and tailored therapies that can improve patient outcomes. Lipid nanocarriers are highly effective drug delivery systems that significantly improve their solubility, bioavailability, and stability while also minimizing unwanted side effects. Surface-modified lipid nanocarriers (liposomes, niosomes, solid lipid nanoparticles, nanostructured lipid carriers, lipid nanocapsules, lipid-polymer hybrid nanocarriers, lipoproteins, and lipoplexes) are employed to improve BBB penetration and uptake through various mechanisms. This systematic review illuminates and covers various topics related to brain malignancies. It explores the different methods of drug delivery used in treating brain malignancies and delves into the benefits, limitations, and types of brain-targeted lipid-based nanocarriers. Additionally, this review discusses ongoing clinical trials and patents related to brain malignancy therapies and provides a glance into future perspectives for treating this condition.

Advance and opportunities in nanoparticle drug delivery for central nervous system disorders: A review of current advances

Nanoparticles drug delivery systems have emerged as a cutting-edge approach in treating central nervous system disorders. This review discusses the advancements and opportunities in utilizing nanoparticles for targeted drug delivery to the brain, focusing on their potential to enhance efficacy, reduce side effects, and improve patient outcomes. Lipid-based nanocarriers like liposomes, solid lipid nanoparticles (SLNs) and micelles are widely used in neurological conditions. The growing demand for innovative drug delivery methods for treating neurodegenerative disorders, such as Parkinson's and Alzheimer’s are largely due to potential therapy failures in the blood brain barrier and P-glycoproteins which cause progressive loss of brain function. Nanotechnology advancements can help overcome these limitations by improving the delivery of active medicine campaigns and creating nanomaterials that improve active drug delivery.

Lipid-Based Nanocarrier by Targeting with LHRH Peptide: A Promising Approach for Prostate Cancer Radio-Imaging and Therapy.

Prostate cancer is a prevalently detected malignancy with a dismal prognosis. Luteinizing-hormone-releasing-hormone (LHRH) receptors are overexpressed in such cancer cells, to which the LHRH-decapeptide can specifically bind. A lipid-polyethylene glycol-conjugated new LHRH-decapeptide analogue (D-P-HLH) was synthesized and characterized. D-P-HLH-coated and anticancer drug doxorubicin (DX)-loaded solid lipid nanoparticles (F-DX-SLN) were formulated by the cold homogenization technique and characterized by Fourier transform infrared spectroscopy, X-ray diffraction, X-ray photoelectron spectroscopy, differential scanning calorimetry, dynamic light scattering, electron microscopy, entrapment efficiency, and drug-release profile studies. F-DX-SLN allows site-specific DX delivery by reducing the side effects of chemotherapy. Cancer cells could precisely take up F-DX-SLN by targeting specific receptors, boosting the cytotoxicity at the tumor site. The efficacy of F-DX-SLN on PC3/SKBR3 cells by the MTT assay revealed that F-DX-SLN was more cytotoxic than DX and/or DX-SLN. Flow cytometry and confocal microscopic studies further support F-DX-SLNs' increased intracellular absorption capability in targeting LHRH overexpressed cancer cells. F-DX-SLN ensured high apoptotic potential, noticeably larger mitochondrial transmembrane depolarization action, as well as the activation of caspases, a longer half-life, and greater plasma concentration. F-DX-SLN/DX-SLN was radiolabeled with technetium-99m; scintigraphic imaging studies established its tumor selectivity in PC3 tumor-bearing nude mice. The efficacy of the formulations in cancer treatment, in vivo therapeutic efficacy tests, and histopathological studies were also conducted. Results clearly indicate that F-DX-SLN exhibits sustained and superior targeted administration of anticancer drugs, thus opening up the possibility of a drug delivery system with precise control and targeting effects. F-DX-SLN could also provide a nanotheranostic approach with improved efficacy for prostate cancer therapy.

An Overview on the Physiopathology of the Blood-Brain Barrier and the Lipid-Based Nanocarriers for Central Nervous System Delivery.

The state of well-being and health of our body is regulated by the fine osmotic and biochemical balance established between the cells of the different tissues, organs, and systems. Specific districts of the human body are defined, kept in the correct state of functioning, and, therefore, protected from exogenous or endogenous insults of both mechanical, physical, and biological nature by the presence of different barrier systems. In addition to the placental barrier, which even acts as a linker between two different organisms, the mother and the fetus, all human body barriers, including the blood-brain barrier (BBB), blood-retinal barrier, blood-nerve barrier, blood-lymph barrier, and blood-cerebrospinal fluid barrier, operate to maintain the physiological homeostasis within tissues and organs. From a pharmaceutical point of view, the most challenging is undoubtedly the BBB, since its presence notably complicates the treatment of brain disorders. BBB action can impair the delivery of chemical drugs and biopharmaceuticals into the brain, reducing their therapeutic efficacy and/or increasing their unwanted bioaccumulation in the surrounding healthy tissues. Recent nanotechnological innovation provides advanced biomaterials and ad hoc customized engineering and functionalization methods able to assist in brain-targeted drug delivery. In this context, lipid nanocarriers, including both synthetic (liposomes, solid lipid nanoparticles, nanoemulsions, nanostructured lipid carriers, niosomes, proniosomes, and cubosomes) and cell-derived ones (extracellular vesicles and cell membrane-derived nanocarriers), are considered one of the most successful brain delivery systems due to their reasonable biocompatibility and ability to cross the BBB. This review aims to provide a complete and up-to-date point of view on the efficacy of the most varied lipid carriers, whether FDA-approved, involved in clinical trials, or used in in vitro or in vivo studies, for the treatment of inflammatory, cancerous, or infectious brain diseases.

Preparation and characterization of chitosan-coated noisomal doxorubicin for enhanced its medical application

This study aimed to synthesize and characterize chitosan-coated noisomal doxorubicin for the purpose of enhancing its medical application, particularly in the field of cancer treatment. Doxorubicin, a potent chemotherapeutic agent, was encapsulated within noisomes, which are lipid-based nanocarriers known for their ability to efficiently deliver drugs to target sites. Chitosan, a biocompatible and biodegradable polysaccharide, was used to coat the surface of the noisomes to improve their stability and enhance drug release properties. The synthesized chitosan-coated noisomal doxorubicin was subjected to various characterization techniques to evaluate its physicochemical properties. Transmission electron microscopy (TEM) revealed a spherical structure with a diameter of 500–550 ± 5.45 nm and zeta potential of +11 ± 0.13 mV with no aggregation or agglomeration. Chitosan-coated noisomes can loaded doxorubicin with entrapping efficacy 75.19 ± 1.45%. While scanning electron microscopy (SEM) revealed well-defined pores within a fibrous surface. It is observed that chitosan-coated niosomes loading doxorubicin have optimum roughness (22.88 ± 0.71 nm). UV spectroscopy was employed to assess the drug encapsulation efficiency and release profile. Differential scanning calorimetry (DSC) helped determine the thermal behavior, which indicated a broad endotherm peak at 52.4 °C, while X-ray diffraction (XRD) analysis provided information about the crystallinity of the formulation with an intense peak at 23.79°. Fourier-transform infrared spectroscopy (FTIR) indicated the formation of new bonds between the drug and the polymer. The findings from this study will contribute to the knowledge of the physical and chemical properties of the synthesized formulation, which is crucial for ensuring its stability, drug release kinetics, and biological activity. The enhanced chitosan-coated noisomal doxorubicin has the potential to improve the effectiveness and safety of doxorubicin in cancer treatment, offering a promising strategy for enhanced medical applications.

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.