Lipid Nanocarriers Research Articles

Formulation of benznidazole-lipid nanocapsules: Drug release, permeability, biocompatibility, and stability studies

Benznidazole, a poorly soluble in water drug, is the first-line medication for the treatment of Chagas disease, but long treatment periods at high dosages cause several adverse effects with insufficient activity in the chronic phase. According to these facts, there is a serious need for novel benznidazole formulations for improving the chemotherapy of Chagas disease. Thus, this work aimed to incorporate benznidazole into lipid nanocapsules for improving its solubility, dissolution rate in different media, and permeability. Lipid nanocapsules were prepared by the phase inversion technique and were fully characterized. Three formulations were obtained with a diameter of 30, 50, and 100 nm and monomodal size distribution with a low polydispersity index and almost neutral zeta potential. Drug encapsulation efficiency was between 83 and 92 % and the drug loading was between 0.66 and 1.04 %. Loaded formulations were stable under storage for one year at 4 °C. Lipid nanocapsules were found to protect benznidazole in simulated gastric fluid and provide a sustained release platform for the drug in a simulated intestinal fluid containing pancreatic enzymes. The small size and the almost neutral surface charge of these lipid nanocarriers improved their penetration through mucus and such formulations showed a reduced chemical interaction with gastric mucin glycoproteins. LNCs. The incorporation of benznidazole in lipid nanocapsules improved the drug permeability across intestinal epithelium by 10-fold compared with the non-encapsulated drug while the exposure of the cell monolayers to these nanoformulations did not affect the integrity of the epithelium.

Nanostructured Lipid Carriers for Targeting Central Nervous System: Recent Advancements

Background: Lipid nanocarriers (NLCs) have undergone significant research over the past two decades to determine how well they target drugs to important parts of the human body, such as the central nervous system (CNS), the heart region, tumor cells, etc. Objective: The objective of this review paper was to review and critically summarize recent progress in NLC for targeting CNS. Methods: The structure, classification, elements, and numerous preparation techniques have been carefully outlined in this paper, along with their benefits and drawbacks, as demonstrated by several research investigations. Results: This review focuses on recent developments in NLCs for brain targeting of bioactives with special attention to their surface modifications, formulation aspects, pharmacokinetic behavior, and effectiveness for treating a variety of brain disorders. Conclusion: Poorly water-soluble bioactive substances’ physicochemical properties and behavior, such as aqueous dispersibility and oral bioavailability, can be greatly improved using lipid nanocarriers. Due to the brain's complicated structure and numerous protective systems, drug distribution to the brain has remained a difficult problem for scientists. The employment of an appropriate nanocarrier technology and an alternate drug delivery method, such as nose-to-brain drug delivery, could overcome the problem of brain targeting and increase the therapeutic effectiveness of CNS-acting medications. The pharmaceutical business has recently transformed various innovative drug delivery methods that address the drawbacks of conventional drug delivery systems and offer a good benefit-to-risk ratio.

Prospective Subunit Nanovaccine against Mycobacterium tuberculosis Infection─Cubosome Lipid Nanocarriers of Cord Factor, Trehalose 6,6' Dimycolate.

An improved vaccine is urgently needed to replace the now more than 100-year-old Bacillus Calmette-Guérin (BCG) vaccine against tuberculosis (TB) disease, which represents a significant burden on global public health. Mycolic acid, or cord factor trehalose 6,6' dimycolate (TDM), a lipid component abundant in the cell wall of the pathogen Mycobacterium tuberculosis (MTB), has been shown to have strong immunostimulatory activity but remains underexplored due to its high toxicity and poor solubility. Herein, we employed a novel strategy to encapsulate TDM within a cubosome lipid nanocarrier as a potential subunit nanovaccine candidate against TB. This strategy not only increased the solubility and reduced the toxicity of TDM but also elicited a protective immune response to control MTB growth in macrophages. Both pre-treatment and concurrent treatment of the TDM encapsulated in lipid monoolein (MO) cubosomes (MO-TDM) (1 mol %) induced a strong proinflammatory cytokine response in MTB-infected macrophages, due to epigenetic changes at the promoters of tumor necrosis factor alpha (TNF-α) and interleukin 6 (IL-6) in comparison to the untreated control. Furthermore, treatment with MO-TDM (1 mol %) cubosomes significantly improved antigen processing and presentation capabilities of MTB-infected macrophages to CD4 T cells. The ability of MO-TDM (1 mol %) cubosomes to induce a robust innate and adaptive response in vitro was further supported by a mathematical modeling study predicting the vaccine efficacy in vivo. Overall, these results indicate a strong immunostimulatory effect of TDM when delivered through the lipid nanocarrier, suggesting its potential as a novel TB vaccine.

In vitro/In vivo Evaluation of Elastic Nano-lipid Carriers of Aztreonam for Pneumonic Lungs.

The liposomal inhalation of drugs has been extensively researched for the invasion of biofilms and macrophages in the infected lungs. The present study aimed to explore the in vitro and in vivo effects of elastic nano-lipid vesicles of aztreonam for pulmonary delivery. Elastic nano lipid vesicles of the drug were successfully prepared with the commonly abundant lung phospholipids (LIPOID S PC-3, LIPOID PC 16:0/16:0), cholesterol, and span 20. Four such formulations were evaluated for their physicochemical properties, in vitro diffusion, and cytotoxicity. The best formulation was subjected to stability, in vivo drug deposition on the pneumonic lungs, and histopathological studies. The characterization of the lipid vesicles in terms of particle size, zeta potential, and surface morphology confirmed the formation of stable nanolipid vesicles of the drug. The presence of surfactant in the lipid vesicles exhibited high bilayer stability, entrapment, and diffusion of the drug. The in vitro diffusion study revealed the biphasic characteristic with an initial burst, followed by sustenance for 8 h. A remarkable drug uptake was observed in the epithelial cell line of CHO Cricetulus griseus in the presence of surfactant. The drug was retained on the pneumonic lungs for 8 h. The histopathological study of lung tissue revealed that surfactant-based lipid vesicles could attenuate lung fibrosis significantly. It can be concluded that elastic nano lipid vesicular system of aztreonam could be a paradigm for targeting and localization of the drug with a long residence time in the lungs.

A Critical Appraisal of Lipid Nanoparticles Deployed in Cancer Pharmacotherapy.

Treatment modalities of various cancers and the delivery strategies of anticancer agents have evolved significantly in the recent past. The severity and fatality of the disease and hurdles to the effective delivery of therapeutic agents have drawn the attention of researchers across the world for proposing novel and effective drug delivery strategies for anticancer therapeutics. Attempts have been made to propose solutions to the diverse limitations like poor pharmacokinetics and higher systemic toxicities of the traditional delivery of anticancer agents. Nanotechnology-based drug delivery systems including lipid-based nanocarriers have demonstrated significant efficiency in this scenario. The review critically assessed the different types of lipid nanocarrier systems for the effective and optimal delivery of anticancer therapeutic agents. The diverse synthesis approaches are discussed for the laboratory scale and commercial development of different categories of lipid nanocarriers. Further, their application in anticancer drug delivery is illustrated in detail followed by a critical appraisal of their safety and toxicity.

Physicochemical and In Vitro Digestion Properties of Curcumin-Loaded Solid Lipid Nanoparticles with Different Solid Lipids and Emulsifiers.

Curcumin-loaded solid lipid nanoparticles (Cur-SLN) were prepared using medium- and long chain diacylglycerol (MLCD) or glycerol tripalmitate (TP) as lipid matrix and three kinds of surfactants including Tween 20 (T20), quillaja saponin (SQ) and rhamnolipid (Rha). The MLCD-based SLNs had a smaller size and lower surface charge than TP-SLNs with a Cur encapsulation efficiency of 87.54-95.32% and the Rha-based SLNs exhibited a small size but low stability to pH decreases and ionic strength. Thermal analysis and X-ray diffraction results confirmed that the SLNs with different lipid cores showed varying structures, melting and crystallization profiles. The emulsifiers slightly impacted the crystal polymorphism of MLCD-SLNs but largely influenced that of TP-SLNs. Meanwhile, the polymorphism transition was less significant for MLCD-SLNs, which accounted for the better stabilization of particle size and higher encapsulation efficiency of MLCD-SLNs during storage. In vitro studies showed that emulsifier formulation greatly impacted on the Cur bioavailability, whereby T20-SLNs showed much higher digestibility and bioavailability than that of SQ- and Rha-SLNs possibly due to the difference in the interfacial composition. Mathematical modeling analysis of the membrane release further confirmed that Cur was mainly released from the intestinal phase and T20-SLNs showed a faster release rate compared with other formulations. This work contributes to a better understanding of the performance of MLCD in lipophilic compound-loaded SLNs and has important implications for the rational design of lipid nanocarriers and in instructing their application in functional food products.

Hybrid lipid-biopolymer nanocarrier as a strategy for GBM photodynamic therapy (PDT)

Glioblastoma (GBM) is the most common brain cancer characterized by aggressive and infiltrated tumors. For this, hybrid biopolymer-lipid nanoparticles coated with biopolymers such as chitosan and lipidic nanocarriers (LN) loaded with a photosensitizer (AlClPc) can be used for GBM photodynamic therapy. The chitosan-coated LN exhibited stable physicochemical characteristics and presented as an excellent lipid nanocarrier with highly efficiently encapsulated photosensitizer chloro-aluminum phthalocyanine (AlClPc). LN(AlClPc)Ct0.1% in the presence of light produced more reactive oxygen species and reduced brain tumor cell viability and proliferation. Confirm the effects of in vivo LN applications with photodynamic therapy confirmed that the total brain tumor area decreased without systemic toxicity in mice. These results suggest a promising strategy for future clinical applications to improve brain cancer treatment.

Designing and evaluation of dermal targeted combinatorial nanostructured lipid carrier gel loaded with curcumin and resveratrol for accelerating cutaneous wound healing

A nanostructured lipid carrier containing combined curcumin (CUR) and resveratrol (RSV) was prepared and tested for its potential to accelerate wound healing through topical administration. Prepared nano lipid carrier (NLC) formulation had a particle size of 132.3 ± 4.54 nm, polydispersity index (PDI) of 0.478, and zeta potential of −16.6 mV. Entrapment efficiency (EE) for CUR and RSV was found to be 94.21 ± 0.28% and 84.61 ± 0.15%, respectively. Drug loading was found to be 8.560 ± 0.948% (for CUR) and 7.602 ± 0.452% (for RSV). NLC formulation was converted to NLC gel by incorporation of Carbopol 934 for enhancing its dermal applicability. Flux and permeability coefficient for CUR and RSV in NLC gel was found to be 22.087 µg/cm2/h, 11.299 µg/cm2/h, and 0.2208, 0.1129, respectively, through goat ear skin and 19.213 µg/cm2/h, 22.66 µg/cm2/h and 0.1921, 0.2266, respectively, through Strat-MTM membrane. Dermatokinetic study revealed significant enhancement in Cskin max and AUC0–12h in skin sample treated with NLC gel in comparison with plain gel. Also, NLC gel showed longer retention time which indicates prolonged drug action at targeted site thus, NLC gel may show better therapeutic efficacy than plain gel.

Lipid-based Nanocarriers via Nose-to-Brain Pathway for Alzheimer's and Parkinson's Disease

Abstract: Neurodegenerative disorders are characterized by the progressive, irreversible deterioration of functions of the central nervous system, especially neurons, that lead to cognitive, motor, and intellectual impairment. Alzheimer's disease (AD) and Parkinson's disease (PD) are the most prevalent forms of neurodegenerative disorders and are predicted to be leading causes of mortality. Although conventional formulations are available for symptomatic treatment of AD and PD, many novel formulations and routes of administration are persistently studied for their better management and nose-to-brain delivery is one of them. This platform has been explored with various nanoformulations for targeted brain delivery. Lipid nanocarriers are known for bypassing the blood-brain barrier (BBB) through nasal delivery, and several drugs have been evaluated in the lipid carrier system. This review focuses on various lipid-based nanocarriers such as liposomes, solid lipid nanoparticles, nanostructured lipid carriers, microemulsions, nanoemulsions, micelles and cubosomes reported to treat and alleviate the symptoms of AD and PD via nasal route. It gives an overview of key findings of nasal lipid-based nanocarriers and their improved pharmacokinetic parameters and enhanced neuroprotection that may be utilized in the future to explore it commercially.

Polygonum cuspidatum Loaded Nanostructured Lipid Carriers for Dual Inhibition of TNF-α- and IL-6 Cytokines and Free Radical Species.

The main objective of this study was the testing of natural compounds, such as Polygonum cuspidatum (PgnC) loaded into nanostructured lipid carriers (NLC), which can act as a "double-edged sword" aimed at simultaneously combating dangerous free radicals and inhibiting pro-inflammatory cytokines. Resveratrol-rich PgnC extract was paired with another phytochemical, Diosgenin (DSG), in NLC. The lipid nanocarriers carrying both herbals (NLC-DSG-PgnC) had spherical diameters (100 ± 2 50 nm), a polydispersity index of ~0.15, and electrokinetic potentials greater than -46.5 mV. Entrapment efficiencies of 65% for PgnC and 87% for DSG were determined by chromatographic and UV-Vis spectroscopy assays. Cell cytotoxicity analysis proved that 50 µg/mL of NLC-PgnC and dual-NLC ensured a biocompatible effect like the untreated cells. The dual-NLC assured a much slower in vitro release of DSG and PgnC (67% PgnC and 48% DSG) than the individual-NLC (78% PgnC and 47% DSG) after 4 h of experiments. NLC encapsulating PgnC presented a superior ability to capture cationic radicals: 74.5 and 77.9%. The chemiluminescence results pointed out the non-involvement of DSG in stopping oxygenated free radicals, while the antioxidant activity was maintained at a level higher than 97% for dual-NLC. NLC-DSG-PgnC ensured a promising capacity for inhibition of pro-inflammatory cytokine IL-6, ranging from 91.9 to 94.9%.

Cortisone-loaded stearoyl ascorbic acid based nanostructured lipid carriers alleviate inflammatory changes in DSS-induced colitis.

Ulcerative colitis is a chronic inflammatory disease which poorly affects the colon and spreads toward the rectum over time. Cortisone (CRT) is a corticosteroid clinically used for the management of inflammatory diseases like colitis and other inflammatory bowel diseases. Due to some physicochemical properties' cortisone has limited potency in clinics. To overcome drug-related problems, we successfully prepared lipid nanocarriers with generally regarded as safe (GRAS) materials approved by USFDA. The present study aimed to assess the therapeutic efficacy of CRT-loaded 6-o-stearoyl ascorbic acid (SAA) nanostructured lipid carriers (NLCs) against DSS-induced colitis mice. Formulation and characterizations of reported nanostructured lipid carrier were performed according to our previously optimized parameters. The average hydrodynamic diameter of NLCs was 182nm as measured by DLS with 81.14% encapsulation efficacy. TEM, AFM and SEM images analysis confirmed its spherical appearance. hTERT-BJ cells viability up to a dose of 500μg/ml shows cytocompatible characteristics of blank NLCs. CRT-loaded NLCs treatment normalizes physically observed parameters such as disease activity index, weight variation etc. These NLCs were able to significantly reduce the severity of colitis in terms of colon histoarchitecture, regaining of the goblet cells, mucins secretions, inhibition of proinflammatory cytokines etc. Treatment with CRT-loaded NLCs effectively downregulated the overexpression of inflammatory enzymes like cyclooxygenase-2 (COX-2), Inducible nitric oxide synthase (iNOS) etc. The results of this study concluded that these CRT-encapsulated NLCs efficiently manage the disease severity induced by DSS.

Combining orthogonal measurements to unveil diclofenac encapsulation into polymeric and lipid nanocarriers

The quantification of the drug associated to nanoparticle carriers, often expressed in terms of encapsulation efficiency, is a regulatory requirement. The establishment of independent methods to evaluate this parameter provides a means for measurement validation, which is critical in providing confidence in the methods and enabling the robust characterization of nanomedicines. Chromatography is traditionally used to measure drug encapsulation into nanoparticles. Here, we describe an additional independent strategy based on analytical centrifugation. The encapsulation of diclofenac into nanocarriers was quantified based on the mass difference between placebo (i.e. unloaded) and loaded nanoparticles. This difference was estimated using particle densities measured by differential centrifugal sedimentation (DCS) and size and concentration values measured by particle tracking analysis (PTA). The proposed strategy was applied to two types of formulations, namely poly(lactic-co-glycolic acid) (PLGA) nanoparticles and nanostructured lipid carriers, which were analysed by DCS operated in sedimentation and flotation modes, respectively. The results were compared to those from high performance liquid chromatography (HPLC) measurements. Additionally, X-ray photoelectron spectroscopy analysis was used to elucidate the surface chemical composition of the placebo and loaded nanoparticles. The proposed approach enables the monitoring of batch-to-batch consistency and the quantification of diclofenac association to PLGA nanoparticles from 0.7 ng to 5 ng of drug per 1 μg of PLGA, with good linear correlation between DCS and HPLC results (R2 = 0.975). Using the same approach, similar quantification in lipid nanocarriers was possible for a loading of diclofenac ≥1.1 ng per 1 μg of lipids, with results in agreement with the HPLC method (R2 = 0.971).Hence, the strategy proposed here expands the analytical tools available for evaluating nanoparticles encapsulation efficiency, being thus significant for increasing the robustness of drug-delivery nanocarriers characterization.

Long-term biophysical stability of nanodiamonds combined with lipid nanocarriers for non-viral gene delivery to the retina

Nanodiamonds were combined with niosome, and resulting formulations were named as nanodiasomes, which were evaluated in terms of physicochemical features, cellular internalization, cell viability and transfection efficiency both in in vitro and in in vivo conditions. Such parameters were analyzed at 4 and 25 °C, and at 15 and 30 days after their elaboration. Nanodiasomes showed a particle size of 128 nm that was maintained over time inside the ± 10% of deviation, unless after 30 days of storage at 25 °C. Something similar occurred with the initial zeta potential value, 35.2 mV, being both formulations more stable at 4 °C. The incorporation of nanodiamonds into niosomes resulted in a 4-fold increase of transfection efficiency that was maintained over time at 4 and 25 °C. In vivo studies reported high transgene expression of nanodiasomes after subretinal and intravitreal administration in mice, when injected freshly prepared and after 30 days of storage at 4 °C.

Lipid-Based Nanocarriers in the Treatment of Glioblastoma Multiforme (GBM): Challenges and Opportunities

Glioblastoma multiforme (also known as glioblastoma; GBM) is one of the most malignant types of brain tumors that occurs in the CNS. Treatment strategies for glioblastoma are majorly comprised of surgical resection, radiotherapy, and chemotherapy along with combination therapy. Treatment of GBM is itself a tedious task but the involved barriers in GBM are one of the main impediments to move one step closer to the treatment of GBM. Basically, two of the barriers are of utmost importance in this regard, namely blood brain barrier (BBB) and blood brain tumor barrier (BBTB). This review will address different challenges and barriers in the treatment of GBM along with their etiology. The role and recent progress of lipid-based nanocarriers like liposomes, solid lipid nanocarriers (SLNs), nanostructured lipid carriers (NLCs), lipoplexes, and lipid hybrid carriers in the effective management of GBM will be discussed in detail.

Cubosome Lipid Nanocarriers As a Drug Delivery Vehicle for Intracellular Mycobacterium tuberculosis Infections

Mycobacterium tuberculosis (MTB) causes the infectious disease tuberculosis (TB), responsible for more deaths than any other single infectious disease in history. Intracellular MTB are slow growing and difficult to target with traditional antitubercular drugs, leading to the emergence of multidrug resistance in TB infection, which is a major global public health issue. Recent advances in innovative lipid nanotechnologies for drug delivery have demonstrated promising outcomes for chronic infectious diseases but have not yet been tested as potential delivery systems for intracellular infections such as TB. The current study evaluates the potential of monoolein (MO)-based cationic cubosomes for the encapsulation and delivery of the first line antitubercular drug rifampicin (RIF) against an MTB-H37Ra in vitro culture model. In particular, we show that the use of cationic cubosomes as delivery vehicles reduced the minimum inhibitory concentration (MIC) of RIF by 2-fold against actively replicating MTB-H37Ra (compared to that of the free drug) and also shortened the lifecycle duration of axenic MTB-H37Ra from 5 to 3 days. The cubosome-mediated delivery was also found to be effective against intracellular MTB-H37Ra within THP-1 human macrophages, with a 2.8 log reduction in viability of the bacilli after 6 days incubation at the MIC. The killing time was also reduced from 8 to 6 days without distressing the host macrophages. Mechanistic studies on the uptake of RIF-loaded cationic cubosomes using total internal reflection fluorescence microscopy (TIRFM) demonstrated the capacity of these lipid particles to effectively target intracellular bacteria. Overall, these results demonstrate that cationic cubosomes are a potent delivery system for the antitubercular drug RIF for therapeutic management of TB.

Novel Bovine Serum Albumin-Decorated-Nanostructured Lipid Carriers Able to Modulate Apoptosis and Cell-Cycle Response in Ovarian, Breast, and Colon Tumoral Cells.

A novel nanoscale approach was developed for the improved cellular internalization of hybrid bovine serum albumin-lipid nanocarriers loaded with piperine (NLC-Pip-BSA) in different tumor cells. The effect of the BSA-targeted-NLC-Pip and untargeted-NLC-Pip on the viability, proliferation, and levels of cell-cycle damage and apoptosis in the colon (LoVo), ovarian (SKOV3) and breast (MCF7) adenocarcinoma cell lines was comparatively discussed. NLCs were characterized concerning particle size, morphology, zeta potential, phytochemical encapsulation efficiency, ATR-FTIR, and fluorescence spectroscopy. The results showed that NLC-Pip-BSA showed a mean size below 140 nm, a zeta potential of -60 mV, and an entrapment efficiency of 81.94% for NLC-Pip and 80.45% for NLC-Pip-BSA. Fluorescence spectroscopy confirmed the coating of the NLC with the albumin. By MTS and RTCA assays, NLC-Pip-BSA showed a more pronounced response against the LoVo colon cell line and MCF-7 breast tumor cell lines than against the ovarian SKOV-3 cell line. Flow cytometry assay demonstrated that the targeted NLC-Pip had more cytotoxicity and improved apoptosis than the untargeted ones in MCF-7 tumor cells (p < 0.05). NLC-Pip caused a significant increase in MCF-7 breast tumor cell apoptosis of ~8X, while NLC-Pip-BSA has shown an 11-fold increase in apoptosis.

Solid Lipid Nanoparticles (SLNs): Advancements in Modification Strategies Toward Drug Delivery Vehicle.

Solid lipid nanoparticles are at the cornerstone of the swiftly growing area of medical nanotechnology, having several potential functions in drug delivery, research, clinical care, and a variety of other fields. They provide the opportunity of developing novel therapies due to their unique properties, such as small particle size and being prepared from physiological biodegradable lipids. The loading of bioactive molecules into nanocarriers is a novel drug delivery prototype employed for various drug targeting levels. Hence, SLNs hold a great promise for achieving the aim of targeted and controlled drug delivery. For this reason, they have attracted the extensive attention of scientists and researchers. This review is based on recent studies and research, and here we present advantages, disadvantages, and preparation methods, several advanced modifications, targeting strategies, and recent applications of solid lipid nanocarriers in drug delivery systems.

Tuning Targeted Liposome Avidity to Cells via Lipid Phase Separation.

The addition of both cell-targeting moieties and polyethylene glycol (PEG) to nanoparticle (NP) drug delivery systems is a standard approach to improve the biodistribution, specificity, and uptake of therapeutic cargo. The spatial presentation of these molecules affects avidity of the NP to target cells in part through an interplay between the local ligand concentration and the steric hindrance imposed by PEG molecules. Here, we show that lipid phase separation in nanoparticles can modulate liposome avidity by changing the proximity of PEG and targeting protein molecules on a nanoparticle surface. Using lipid-anchored nickel-nitrilotriacetic acid (Ni-NTA) as a model ligand, we demonstrate that the attachment of lipid anchored Ni-NTA and PEG molecules to distinct lipid domains in nanoparticles can enhance liposome binding to cancer cells by increasing ligand clustering and reducing steric hindrance. We then use this technique to enhance the binding of RGD-modified liposomes, which can bind to integrins overexpressed on many cancer cells. These results demonstrate the potential of lipid phase separation to modulate the spatial presentation of targeting and shielding molecules on lipid nanocarriers, offering a powerful tool to enhance the efficacy of NP drug delivery systems.

Perspectives on cutting-edge nanoparticulate drug delivery technologies based on lipids and their applications.

Numerous nanotech arenas in therapeutic biology have recently provided a scientific platform to manufacture a considerable swath of unique chemical entities focusing on drugs. Recently, nanoparticulate drug delivery systems have emerged to deliver a specific drug to a specified site. Among all other carriers, lipids possess features exclusive to nanostructured dosage forms. The bioavailability of orally administered drugs is typically negatively affected by their poor water solubility, resulting from the unique chemical moieties introduced. Because of their unique advantages, lipid nanoparticles must become increasingly predictable as a robust delivery mechanism. The enhanced biopharmaceutical properties and significance of lipid-based targeting technologies such as liposomes, niosomes, solid lipid nanoparticles and micelles are highlighted in this review. Pharmaceutical implications of lipid nanocarriers for the transport and distribution of various therapeutic agents, such as biotechnological products and small pharmaceutical molecules, is a booming topic. Lipid nanoparticles as drug delivery systems have many appealing properties, including high biocompatibility, ease of preparation, tissue specificity, avoidance of reticuloendothelial systems, delayed drug release, scale-up feasibility, nontoxicity and targeted delivery. The use of lipid nanoparticles to enhance the transport of biopharmaceuticals is currently considered state-of-the-art. Similarly, we critically examine the upcoming guidelines that therapeutic scientists should handle.

Neutral Oil-Incorporated Liposomal Nanocarrier for Increased Skin Delivery of Ascorbic Acid

In this study, a neutral oil-incorporated liposomal system (lipo-oil-some, LOS) was designed to improve the skin absorption of ascorbic acid (Vit C), and the effects of an edge activator and neutral oil on the skin absorption of Vit C were evaluated. As components of the LOS system, sodium deoxycholate, polysorbate 80, and cholesterol were screened as edge activators, and camellia oil, tricaprylin, and grapeseed oil were employed as neutral oils. The LOS systems prepared by the ethanol injection method were spherical in shape, 130-350 nm in size, and had 4-27% Vit C loading efficiency (%). In a skin absorption study using a Franz diffusion cell mounted with porcine skin, the LOS system prepared with sodium deoxycholate (10 w/w% of phospholipid) exhibited 1.2-and 2.9-fold higher absorption than those prepared with polysorbate 80 and cholesterol, respectively. Moreover, the type of neutral oil had a marked effect on the absorption of Vit C; the liposomal system containing camellia oil provided 1.3 to 1.8 times higher flux (45.4 μg/cm2∙h) than vesicles with tricaprylin or grapeseed oil, respectively. The optimized lipid nanocarrier is expected to be a promising tool for promoting the skin absorption of Vit C and improving its dermatological functions.