Advances in the application of lipid nanocapsules and nanostructured carriers in the treatment of lung cancer.

Lipid nanocapsules for dermal application: A comparative study of lipid-based versus polymer-based nanocarriers

Hydrophilic drugs are proficient therapeutic drug candidates; however, their effective delivery poses a formidable challenge. Therefore, the development of an efficient drug delivery system demands a multifaceted approach. In recent decades, nanolipid carriers have emerged as promising drug delivery systems, offering enhanced stability, improved bioavailability, and controlled release profiles. Although nanolipid carriers have been widely investigated as carriers for hydrophobic drugs and have demonstrated remarkable success in encapsulating hydrophobic drugs, encapsulating a hydrophilic drug moiety still remains a challenge. The current study provides a comprehensive review of innovative methods developed for the successful encapsulation of hydrophilic drugs into nanolipid carriers. The first section of the study explores the physicochemical properties of hydrophilic drugs and the inherent challenges associated with their encapsulation in lipid-based carriers. The subsequent sections delve into the various strategies employed to overcome these challenges. Emphasis is placed on novel formulation techniques investigated for the encapsulation of hydrophilic drugs into nano lipid carriers. The present review not only delineates the various traditional methods for high entrapment of hydrophilic drugs but also underscores modifications to the hydrophilic drug candidates, facilitating their efficient encapsulation into nanolipid carrier drug carriers. This study explores the current state of knowledge regarding methods for encapsulating hydrophilic drugs into nanolipid carriers. By addressing the challenges associated with hydrophilic drug encapsulation and presenting innovative strategies, this review aims to provide valuable insights to researchers and pharmaceutical scientists working in the field of nanomedicine and drug delivery.

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.

Drug delivery technology has a wide spectrum, which is continuously being upgraded at a stupendous speed. Lipid nanocarriers have emerged as a very promising, emerging and rapidly developing tool for the delivery of various drugs lacking solubility, bioavailability and stability in the recent couple of decades. Recent studies show that about 40% of newer drugs have such problems. Initially, a lipid carrier was denoted by the liposome and similar vesicular systems, but currently they are categorized as colloidal nano lipid-based carriers (CNLBC). To avoid the limitation of these CNLBCs in pH- and enzyme-dependent degradation, especially when taken orally or in physical and chemical-related stability issues, newer lipid nanocarriers such as solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLCs), lipid drug conjugates (LDCs), and pharmacosomes have shown their importance at greater extent due to low toxicity, improved bioavailability, high biocompatibility, high drug-loading efficiency, protection from degradation in GIT, etc. . 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. Lipid nanocarriers can load both hydrophilic and lipophilic drug. Solubility is a rate-limiting step in the case of lipophilic drugs (BCS Class II and IV), which can be greatly modified by formulation of lipid nanocarriers. Similarly, lipidic nanocarriers can increase the permeability of most of the hydrophilic drugs (BCS I and III class) which is the rate limiting step this case. These carriers also shows good controlled and target specific drug delivery system which always attracts the attention of researchers.The current chapter aims to present a special concern related to various types of lipid nanocarriers, their detailed description on composition, different methods of preparation, influence of various types of lipids on the different properties of such carriers. It also covers the various physicochemical, formulation, pharmacokinetic, and cytotoxic aspects of such carriers. Furthermore, it includes the marketed formulations of lipid nanocarriers with their company name and trade name.

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.

Lipid-based nanocarriers have emerged as promising vehicles for the delivery of various therapeutic agents, owing to their biocompatibility, stability, and ability to encapsulate both hydrophilic and hydrophobic drugs. Among these lipid-based nanocarriers, Solid Lipid Nanoparticles (SLNs) and Nanostructured Lipid Carriers (NLCs) have gained significant attention in the field of drug delivery. This comparative review aims to provide a comprehensive analysis of SLNs and NLCs, focusing on their formulation, physicochemical properties, drug-loading capacity, stability, and drug release profiles. The review highlights the differences in preparation techniques, particle size, zeta potential, drug encapsulation efficiency, stability, drug delivery, cosmetic and personal care, and food industry applications between SLN and NLC. Furthermore, the review discusses the toxicity and safety profiles of these nanoparticles, including cytotoxicity, genotoxicity, acute toxicity, and long-term toxicity. Finally, the review identifies the potential applications, limitations, and future research directions of SLN and NLC.In summary, this comparative review provides valuable insights into the formulation, physicochemical properties, drug-loading capacity, stability, and drug release profiles of SLNs and NLCs. By understanding the similarities and differences between these lipid-based nanocarriers, researchers and pharmaceutical scientists can make informed decisions regarding the selection of the most suitable nanocarrier for specific therapeutic applications.

Curcumin is a unique molecule naturally obtained from rhizomes of Curcuma longa. Curcumin has been reported to act on diverse molecular targets like receptors, enzymes, and co-factors; regulate different cellular signaling pathways; and modulate gene expression. It suppresses expression of main inflammatory mediators like interleukins, tumor necrosis factor, and nuclear factor κB which are involved in the regulation of genes causing inflammation in most skin disorders. The topical delivery of curcumin seems to be more advantageous in providing a localized effect in skin diseases. However, its low aqueous solubility, poor skin permeation, and degradation hinder its application for commercial use despite its enormous potential. Lipid-based nanocarrier systems including liposomes, niosomes, solid lipid nanoparticles, nanostructured lipid carriers, lyotropic liquid crystal nanoparticles, lipospheres, and lipid nanocapsules have found potential as carriers to overcome the issues associated with conventional topical dosage forms. Nano-size, lipophilic nature, viscoelastic properties, and occlusive effect of lipid nanocarriers provide high drug loading, hydration of skin, stability, enhanced permeation through the stratum corneum, and slow release of curcumin in the targeted skin layers. This review particularly focuses on the application of lipid nanocarriers for the topical delivery of curcumin in the treatment of various skin diseases. Furthermore, preclinical studies and patents have also indicated the emerging commercialization potential of curcumin-loaded lipid nanocarriers for effective drug delivery in skin disorders. Graphical Abstract.

Lipid nanocarriers have recently arisen with a wide range of uses and research areas, with the advantages they offer in virtue of their unique properties. They are easily synthesized, scaled up, biodegradable, proper to transport many bioactive components, have a high loading capacity, and are convenient for various routes of administration (parenteral, oral, dermal, ocular, etc.). These carriers overcome the problems of bioactive substances such as low solubility, plasma half-life and bioavailability, and side effects, as well as providing controlled release, local delivery, and targeting. Lipid-based nanoparticular systems can be categorized into two basic classes, vesicular and non-vesicular. While liposomes are the most widely used vesicular structures, solid lipid nanoparticles and nano-structured lipid carriers are non-vesicular nanocarriers. These nanocarriers have many medical uses, such as cancer therapy, gene therapy, photodynamic therapy, treatment of infectious diseases and neurodegenerative diseases, vaccines, imaging, etc. It is essential that the synthesis method of lipid-based nanocarriers and the components from which they are composed are selected in accordance with the medical application area and characterization studies are carried out. In this article, liposomes, solid lipid nanoparticles and nano-structured lipid carriers will be discussed as lipid-based nanocarriers, synthesis and characterization methods will be emphasized and examples from medical applications will be given.

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.

The digestion behaviour of lipid-based nanocarriers (LNC) has a great impact on their oral drug delivery properties. In this study, various excipients including surfactants, glycerides and waxes, as well as various drug-delivery systems, namely self-emulsifying drug delivery systems (SEDDS), solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were examined via the pH-stat lipolysis model. Lipolysis experiments with lipase and pancreatin revealed the highest release of fatty acids for medium chain glycerides, followed by long chain glycerides and surfactants. Waxes appeared to be poor substrates with a maximum digestion of up to 10% within 60 min. Within the group of surfactants, the enzymatic cleavage decreased in the following order: glycerol monostearate > polyoxyethylene (20) sorbitan monostearate > PEG-35 castor oil > sorbitan monostearate. After digestion experiments of the excipients, SEDDS, SLN and NLC with sizes between 30 and 300 nm were prepared. The size of almost all formulations was increasing during lipolysis and levelled off after approximately 15 min except for the SLN and NLC consisting of cetyl palmitate. SEDDS exceeded 6000 nm after some minutes and were almost completely hydrolysed by pancreatin. No significant difference was observed between comparable SLN and NLC but surfactant choice and selection of the lipid component had an impact on digestion. SLN and NLC with cetyl palmitate were only digested by 5% whereas particles with glyceryl distearate were decomposed by 40–80% within 60 min. Additionally, the digestion of the same SLN or NLC, only differing in the surfactant, was higher for SLN/NLC containing polyoxyethylene (20) sorbitan monostearate than PEG-35 castor oil. This observation might be explained by the higher PEG content of PEG-35 castor oil causing a more pronounced steric hindrance for the access of lipase. Generally, digestion experiments performed with pancreatin resulted in a higher digestion compared to lipase. According to these results, the digestion behaviour of LNC depends on both, the type of nanocarrier and on the excipients used for them.

Among the colloidal vectors proposed for the controlled delivery and targeting of drugs and other biologically active compounds, lipid-based nanocarriers are acquiring an increasing role due to a number of peculiar technological and physical features. Solid lipid nanoparticles, lipid nanocapsules, nanostructured lipid carriers, and drug-lipid conjugates are all examples of how it can be possible to combine the properties of the more acknowledged liposomal systems, such as biocompatibility and biodegradability, with the stability and compositional flexibility, distinctive of polymeric nanosystems. This article introduces recent patents, filed in years 2007-2013, that deal with novel or amended methods of production of the various types of lipid-based nanocarriers. Although a significant gap still remains between basic research and patenting activity in this field, many of the proposed methods can attain an industrial value. Furthermore, the critical analysis of these patents further supports the position that a general revision of patenting systems at an international level would be necessary for nanosized pharmaceutical systems.

Schizophrenia is a persistent and incapacitating neuropsychiatric condition that presents considerable obstacles regarding pharmacological administration and therapeutic effectiveness. Lipidic nanocarriers, including Solid Lipid Nanoparticles (SLNs) and Nanostructured Lipid Carriers (NLCs), have emerged as effective drug delivery vehicles for enhancing the bioavailability, stability, and controlled release of antipsychotic medicines. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) have several benefits, such as improved drug loading capacity, less systemic adverse effects, and superior efficacy in traversing the blood-brain barrier compared to conventional formulations. This study examines advancements in the development of solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) for schizophrenia therapy, emphasising their potential to improve cerebral medication delivery, extend drug release duration, and decrease administration frequency. Moreover, the essay discusses the difficulties related to the scaling of lipid-based nanocarriers, regulatory obstacles, long-term safety concerns, and the necessity for personalised treatment strategies. Notwithstanding the encouraging results in preclinical models, other challenges persist, including the necessity for enhanced formulation methodologies, safety validation, and regulatory clarity. Future possibilities entail the advancement of personalised nanomedicine platforms and intelligent nanocarriers that respond to particular stimuli, perhaps transforming schizophrenia treatment through more targeted, efficient, and individualised treatments.

Lipid nanocarriers show occlusive properties that may be related to their ability to improve skin hydration. The aim of this work was to evaluate the relationship between in vitro occlusion factor and in vivo skin hydration for three types of lipid nanocarriers: nanoemulsions (NEs), solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs). These lipid nanocarriers were loaded with trans-resveratrol (RSV) and incorporated in gel vehicles. In vitro occlusion factor was in the order SLNs > NLCs > NEs. Gels containing unloaded or RSV loaded lipid nanocarriers were applied on the back of a hand of 12 healthy volunteers twice a day for one week, recording skin hydration changes using the instrument Soft Plus. An increase of skin hydration was observed for all lipid nanocarriers (SLNs > NLCs > NEs). RSV loading into these nanocarriers did not affect in vitro and in vivo lipid nanocarriers effects. A linear relationship (r2 = 0.969) was observed between occlusion factor and in vivo increase of skin hydration. Therefore, the results of this study showed the feasibility of using the occlusion factor to predict in vivo skin hydration resulting from topical application of different lipid nanocarriers loading an active ingredient with no inherent hydrating activity.

Acne vulgaris is a prevalent dermatological condition resulting from inflammation, follicular hyperkeratinization, and bacterial growth. Standard treatments, whether topical or oral, frequently encounter challenges such as limited skin penetration, drug instability, and undesirable side effects. The report found that lipid-based nanocarriers have emerged as a promising alternative, demonstrating the potential for enhanced therapeutic effectiveness, better skin bioavailability, controlled drug release, and targeted delivery specifically to sebaceous glands, which help minimize systemic side effects. This review article aims to explore the therapeutic potential of various lipid nanocarriers, including Solid Lipid Nanoparticles (SLNs), Nanostructured Lipid Carriers (NLCs), liposomes, microemulsions, niosomes, and ethosomes particularly by examining the mechanisms through which they penetrate the stratum corneum and deeper skin layers to enhance drug delivery. This review comprehensively surveys lipid-based nanocarriers for acne vulgaris treatment, drawing from a systematic literature search across Google Scholar, Science Direct, Scopus, Web of Science, and PubMed for publications between 2015 and 2025. The search strategy employed keywords such as "lipid nanocarrier," "acne vulgaris," "animal models," or "preclinical studies," and "clinical trials" to capture the research landscape. The review compiles evidence from multiple preclinical experiments and clinical trials regarding the effectiveness of lipid nanocarriers in managing acne. It explores the different pathways these lipid nanocarriers use to permeate the skin and reach target sites. Additionally, it also covers different patents filed by various researchers focusing on the application of lipid nanocarriers for acne management. Lipid nanocarriers represent a significant advancement in dermatological drug delivery, particularly for acne management. By leveraging various skin penetration mechanisms to improve drug targeting to the pilosebaceous unit, they offer potential for more effective treatment compared to conventional methods. While promising, ongoing research and development are necessary to overcome current limitations and fully harness the potential of lipid nanocarriers in clinical practice.