Ethanol Injection Method Research Articles

Preparation of Topical Nano Gel Loaded With Hesperidin Emusomoes: In vitro and in vivo Studies

Objectives: The objective of the present study was to increase the solubility of poorly soluble drug hesperidin and to increase the efficacy of the drug by loading hesperidin in emulsomal topical gel. Methods: Hesperidin was loaded into emulsomes by using ethanol injection method. The optimized formulation of emulsomes was evaluated by SEM, FT-IR, DSC, P-XRD, in vitro drug release, ex-vivo skin permeation studies, in vivo pharmacokinetic and pharmacodynamic studies. Results: The SEM study shows the emulsomes were tiny and spherical in structure. The particle size and zeta potential of the optimized formulation was found to be 50nm and -1.8mV and in vitro drug release was found to be 98.6% for 6 hrs. The optimized emulgel was prepared by using different gelling agents Carbopol 934 and HPMC. The prepared gels were found to be homogenous and skin permeation studies was found to be 98.9% for 4 hr, with skin permeation efficacy bearing flux value 12.3μg/cm2/h when compared to the pure hesperidin gel. The in vivo pharmacokinetic and pharmacodynamic studies were found to be more efficient for the hesperidin loaded emulsomal gel when compared to the marketed formulation. Conclusion: Hesperidin emulsomal gel has shown a significant increase (p<0.05) in activity when compared to the marketed formulation.

Development of Antioxidant-Loaded Nanoliposomes Employing Lecithins with Different Purity Grades.

This work focused on comparing the ability of lecithins with two purity grades regarding their performance in the development of nanoliposomes, as well as their ability to contain and release polar (trans-aconitic acid) and non-polar (quercetin) antioxidant compounds. First, the chemical characterization of both lecithins was carried out through infrared spectroscopy (FTIR), electrospray ionization mass spectrometry (ESI/MS), and modulated differential scanning calorimetry (mDSC). Second, nanoliposomes were prepared by the ethanol injection method and characterized by means of particle size, polydispersity, and zeta potential measurements. Third, the encapsulation efficiency and in vitro release profiles of antioxidants were evaluated. Finally, the antioxidant effect of quercetin and trans aconitic acid in the presence and absence of nanoliposomes was assessed through the oxygen radical absorbance capacity (ORAC) assay. The results showed that, although there are differences in the chemical composition between the two lecithins, these allow the development of nanoliposomes with very similar physicochemical features. Likewise, nanoliposomes elaborated with low purity grade lecithins favored the encapsulation and release of trans-aconitic acid (TAA), while the nanoliposomes made with high purity lecithins favored the encapsulation of quercetin (QCT) and modified its release. Regarding the antioxidant effect, the vehiculization of TAA and QCT in nanoliposomes led to an increase in the antioxidant capability, where QCT showed a sustained effect over time and TAA exhibited a rapidly decaying effect. Likewise, liposomal systems were also found to have a slight antioxidant effect.

Nanoliposomes as delivery system for anthocyanins: Physicochemical characterization, cellular uptake, and antioxidant properties

Anthocyanins (ACNs) are a series of polyphenols found in plants with various biological activities. To overcome their instability toward external environments and provide more effective encapsulation method, anthocyanins-loaded nanoliposomes (AN) were firstly prepared by combining ethanol injection method with ultrasonication. This method was simple and safe which avoiding organic solvents. Good physicochemical characterizations of AN (0.15% w/v ACNs) including the encapsulation efficiency (EE, 91.1 ± 1.7%), mean particle size (53.8 ± 1.8 nm), ζ-potential (−42.7 ± 2.2 mV) and polydispersity index (PDI, 0.19 ± 0.02) were observed. The encapsulation of AN was confirmed by transmission electron microscopy (TEM), differential scanning calorimetry (DSC) and fourier transform infrared (FTIR) spectroscopy. Nanoliposome encapsulation also enhanced the stability, cellular uptake and antioxidant activities of ACNs in vitro. It was demonstrated that the nanoliposomes prepared by this method were an efficient carriers for the delivery of ACNs, and the results expects to provide theories and practice guides for further applications of AN.

Oleosomes Encapsulating Sildenafil Citrate as Potential Topical Nanotherapy for Palmar Plantar Erythrodysesthesia with High Ex vivo Permeation and Deposition.

Palmar plantar erythrodysesthesia (PPE) is a commonly reported skin toxicity of chemotherapeutic agents that significantly affects patients' quality of life. PPE is described as inflammation, swelling, and even cracks and ulcers in the skin of palms and soles of the feet. Conventional treatment includes topical creams, analgesics, or corticosteroids. However, serious cases are not responding to these medications. PPE has been reported to cause drug cessation or dose reduction if not properly treated. Sildenafil citrate (SC) has a well-documented activity in wound healing through improving blood supply to the affected area. However, SC has poor physicochemical properties limiting its transdermal permeation and deposition. This research endeavored to elaborate novel vesicular system with natural components, phospholipids and oleic acid, loaded with sildenafil citrate for topical management of PPE. Sildenafil-loaded oleosomes were prepared using modified ethanol injection method. Optimized oleosomes had nanometric particle size (157.6nm), negative zeta potential (- 85.2 mv), and high entrapment efficiency (95.56%). Ex vivo studies on human skin revealed that oleosomes displayed 2.3-folds higher permeation and 4.5-folds more deposition through the human skin compared to drug suspension. Results endorsed SC oleosomes as suitable topical treatment of PPE providing ameliorated sildenafil permeability in addition to acting as a reservoir for gradual release of the drug. Graphical abstract.

Continuous-Flow Production of Liposomes with a Millireactor under Varying Fluidic Conditions.

Continuous-flow production of liposomes using microfluidic reactors has demonstrated advantages compared to batch methods, including greater control over liposome size and size distribution and reduced reliance on post-production processing steps. However, the use of microfluidic technology for the production of nanoscale vesicular systems (such as liposomes) has not been fully translated to industrial scale yet. This may be due to limitations of microfluidic-based reactors, such as low production rates, limited lifetimes, and high manufacturing costs. In this study, we investigated the potential of millimeter-scale flow reactors (or millireactors) with a serpentine-like architecture, as a scalable and cost-effective route to the production of nanoscale liposomes. The effects on liposome size of varying inlet flow rates, lipid type and concentration, storage conditions, and temperature were investigated. Liposome size (i.e., mean diameter) and size dispersity were characterised by dynamic light scattering (DLS); z-potential measurements and TEM imaging were also carried out on selected liposome batches. It was found that the lipid type and concentration, together with the inlet flow settings, had significant effects on the properties of the resultant liposome dispersion. Notably, the millifluidic reactor was able to generate liposomes with size and dispersity ranging from 54 to 272 nm, and from 0.04 to 0.52 respectively, at operating flow rates between 1 and 10 mL/min. Moreover, when compared to a batch ethanol-injection method, the millireactor generated liposomes with a more therapeutically relevant size and size dispersity.

Assessment of Immunostimulating effect of Carica papaya-based Immunostimulatory Complexes Against Streptococcus pneumoniae Infections

Objectives: Streptococcus pneumoniae infection is a bacterial infection responsible for one-fifth of child mortality in Africa. The aim of this study was to formulate and evaluate Carica papaya-based Immunostimulatory complexes against Streptococcus pneumoniae infections. Methods: Leaves of the plant were harvested, air-dried, pulverized and the saponin content extracted using distilled water and but anole in a Soxhlet’s apparatus. The formulation of Immunostimulatory complexes was prepared using the ethanol injection method. Acute toxicity test and Immunological assays, namely: neutrophil adhesion, carbon clearance, hem agglutinating antibody titer were conducted using healthy laboratory mice. The results were compared to standard drug (levamisole). Results: The aqueous extract and butanol fraction yielded 7.45% and 0.38% saponin. At 5000mg/ kg body weight of administered immunostimulatory complexes, no death or behavioral changes were recorded. Neutrophil adhesion showed no significant increase (20.82±4.34) as against the levamisole (20.74±3.31). The increased phagocytic index (0.089± 0.017) showed better stimulation of reticuloendothelial system when compared to both controls (distilled water = 0.032 ± 0.001; levamisole = 0.071 ± 0.001).The lower Hemagglutination antibody titre value indicates the potency of the formulated ISCOM to elicit an immune response. The ISCOM dose (250 mg/kg body weight) significantly elevated hemagglutination antibody titre (7.81±1.60). Conclusion: It can be inferred from this study that Carica papaya leaves has immunomodulatory capacity and has significant saponin yield which could potentially serve as a component of Immunostimulatory complexes formulation. Carica papaya-based Immunostimulatory complexes exhibit improved immunogenicity against Streptococcus pneumoniae infections.

Enrichment of dark chocolate with vitamin D3 (free or liposome) and assessment quality parameters.

Liposomes are suitable carrier for bioactive components. Ethanol injection method was chosen for preparation liposomes included vitamin D3 for addition into dark chocolate [5µg/serving (10g)]. Assessment the quality of prepared liposomes were performed by measurement particle size distribution, zeta potential, loading efficiency and FTIR. Loading efficiency was 62.58 ± 1.2%. It could be concluded the chosen method for liposome preparation was suitable. In vitro release of vitamin D3 from liposome structure showed the release follow Korsmeyer-Peppas model. Fortified chocolate properties included Differential Scanning Calorimeter (DSC), color indexes, casson viscosity and sensory properties were evaluated. According to the results, there was no significant changes in all tested properties in fortified chocolate than control sample. Vitamin D3 retention during storage time (0, 15, 30, 45, 60 and 70days) were evaluated and results revealed there was better retention of vitamin D3 in fortified samples with liposomes than free vitamin D3. Observation showed addition both forms of vitamin D3 (free or liposome) had no significant impact on color indexes, rheological properties, DSC parameters as well as sensory characteristics.

Vitamin D3 Loaded Niosomes and Transfersomes Produced by Ethanol Injection Method: Identification of the Critical Preparation Step for Size Control.

Vesicular nanocarriers have an important role in drug delivery and dietary supplements. Size control and optimization of encapsulation efficiency (EE) should be optimized for those applications. In this work, we report on the identification of the crucial step (injection, evaporation, or sonication) innanovesicles (transfersomes and niosomes) preparation by theethanol injection method (EI). The identification of each production step on the final vesicle size was analyzed in order to optimize further scale-up process. Results indicated that the final size of transfersomeswas clearly influenced by the sonication step while the final size of niosomes was mainly governed by the injection step. Measurements of final surface tension of the different vesicular systems prepared indicate a linear positive tendency with the vesicle size formed. This relation could help to better understand the process and design a vesicular size prediction model for EI. Vitamin D3 (VitD3) was encapsulated in the systems formulated with encapsulation efficiencies larger than 90%. Interaction between the encapsulated compound and the membrane layer components is crucial for vesicle stability. This work has an impact on the scaling-up production of vesicles for further food science applications.

Formulation and evaluation of baclofen liposome vesicles using lecithin

Introduction: The main aim of present study was to prepare and characterize liposomal formulation of baclofen to improve the effectiveness of the topically applied formulation. Method: For the preparation of liposomes, different ratio of lecithin, cholesterol and ethanol were taken but ratio of drug and stearic acid were kept constant and prepared by ethanol injection method. Liposomes were characterized for vesicle size, vesicle shape, entrapment efficiency, in vitro studies, stability studies and in vivo studies. Results: The average particle size of formulated liposome was in the range of 3.98±0.45-4.24±0.65 µm and small unilamellar vesicles with spherical in shape observed. Entrapment efficiency of optimized formulation was 58.67±0.81 %. The maximum % cumulative drug release behaviours were 67.66±5.32 % after 10 h. formulation stored in 4±2 °C temperature shows better stability (64.19±0.26) compared to elevated temperature. Swiss albino mice were used for the in vivo study and exhibit muscle relaxant activity in terms of no. of falls from rota rod apparatus (p value =0.001). Conclusions: Baclofen loaded liposomal formulation have shown skeletal muscle relaxant activity in mice suggesting delivery of baclofen from liposomes in the therapeutic range.

Improvement of the multi-performance biocharacteristics of cordycepin using BiloNiosome-core/chitosan-shell hybrid nanocarriers

Cordycepin, a derivative of the nucleotide adenosine, has displayed several pharmacological activities including enhanced apoptosis and cancer cells inhibition. However, oral administration of cordycepin has limited practical use due to its poor bioavailability in the intestine. Herein, we developed and demonstrated a hybrid nanocarrier system in the form of biloniosome-core/chitosan-shell hybrid nanocarriers (HNCs) in order to improve the bio-characteristics of cordycepin. In this study, HNCs were prepared by using a solvent (ethanol) injection method involving cordycepin as the biloniosome core and mucoadhesive chitosan biopolymer as a coating shell. Our results showed that the cordycepin-loaded HNCs were positively charged with enhanced mucoadhesive characteristics and highly stable in gastric fluid. The increased permeability of cordycepin-loaded HNCs compared with standard cordycepin was confirmed by in vitro intestinal permeation study across the human intestinal barrier. In addition, we demonstrated that the cordycepin-loaded HNCs are able to release their components in an active form resulting in enhanced anti-cancer activity in two-dimensional (2D) cell cultures as well as in three-dimensional (3D) multi-cellular spheroids of colon cancer cells. Further, quantitative real time PCR analysis of apoptotic gene expression revealed that cordycepin HNCs can induce apoptosis in cancer cells by negatively regulating the expression of B-cell lymphoma-extra large (BCL-XL). I Overall our results showed that the hybrid nanocarrier systems represent a promising strategy for improving the bio-characteristics of cordycepin which can be considered as a potential anti-cancer agent for colorectal cancer chemotherapy.

Experimental Design Supported Liposomal Aztreonam Delivery: In Vitro Studies.

Purpose: The present study focuses on a systemic approach to develop liposomal aztreonam as a promising dosage form for inhalation therapy in the treatment of pneumonia and explores the in-vitro antimicrobial and cell uptake efficacy. Methods: Liposomes were prepared by ethanol injection method using the lipids - soya phosphatidylcholine (SP) and cholesterol (CH). A central composite design (CCD) was employed to optimize the lipid composition to evaluate the effect on vesicle size, zeta potential and entrapment efficiency of the formulation. A numerical and graphical optimization was carried out to predict the optimized blend. The optimized formulation was characterized for vesicle size, surface charge, encapsulation, surface morphology, differential scanning calorimetry (DSC), powder X Ray Diffraction (PXRD), thermogravimetric analysis (TGA), in vitro diffusion, accelerated stability studies, antimicrobial studies on Pseudomonas aeruginosa NCIM 2200 and in vitro cell uptake studies. Results: The optimized formulation was found to have a particle size of 144 nm, a surface charge of -35 mV, with satisfactory drug entrapment. The surface morphology study proved the formation of nanosized vesicles. The drug release from liposomal matrix was biphasic in nature. The solid-state study revealed the reason for good encapsulation of drug. The moisture retention capacity was found to be minimum. The anti-microbial study revealed the potential antibacterial activity of the optimized formulation over the pure drug. The formulation was found to be safe on the epithelial cells and showed a marked increase in cellular uptake of aztreonam in a lipid carrier. Conclusion: It can be concluded that the optimized liposomal aztreonam could be considered as a promising approach for the delivery of aztreonam through inhalation.

Nanoliposome Precursors for Shape Modulation: Use of Heuristic Algorithm and QBD Principles for Encapsulating Phytochemicals.

Screening of multiple methods is worthless for formulators due to material losses, wastage of time, and expenditures. It is imperative to make a quick decision. The present investigation describes the systematic approach to select the best suitable method for the development of nanoliposomes (NL), the precursor of nanocochleates encapsulating curcumin using Analytic Hierarchy Process (AHP). Pair-wise comparison matrices were used to achieve the overall priority weight and ranking for the selection of appropriate technique. Furthermore, Plackett-Burman screening Design (PBD) was exploited to investigate specific effects of associated formulation and process variables on particle size (Y1), drug content (Y2), and entrapment efficiency (Y3), while fabricating NL. Results revealed the reliability of the pair-wise comparison matrices and selected the ethanol injection method with the highest priority weight (0.337). Bland-Altman plot and control chart validated the results of AHP. The preparation of vesicles with the preferred diameter and size distribution was essentially fulfilled. Stirring speed (X5), amount of phospholipid (X4), and cholesterol (X8) showed significant influence (p<0.05;) on Y1 and Y3, PBD revealed. These factors can be further optimized using the design of experiments. AHP being an effective tool, has assisted in selecting the best alternative for fabricating NL, whilst PBD enabled a clear understanding of the effects of diverse formulation variables on responses studied. Results ensure that NL is a riveting candidate for modulating effectively into tailormade diverse shaped nanoformulations for further in vitro; and in vivo; studies.

Formulation of Sodium Valproate Nanospanlastics as a Promising Approach for Drug Repurposing in the Treatment of Androgenic Alopecia

Sodium valproate (SV) is an antiepileptic drug that is widely used in the treatment of different seizure disorders. The topical SV has a hair regenerative potential through activating the Wnt/β-catenin pathway and anagen phase induction. The aim of the current investigation was to fabricate nanospanlastics of SV for improving its dermal delivery by providing prolonged drug effect and increasing its permeability for treatment of androgenic alopecia (AGA). SV-loaded nanospanlastics were formulated according to 23 factorial design by ethanol injection method using a non-ionic surfactant (Span 60) and edge activators (EAs), such as Tween 80 and Cremophor RH 40, to explore the influence of different independent variables on entrapment efficiency (EE%) and percentage drug released after 12 h (Q12h) in order to choose the optimized formula using Design-Expert software. The optimized formula (F8) appeared as spherical deformable vesicles with EE% of 90.32 ± 2.18% and Q12h of 90.27 ± 1.98%. F8 exhibited significant improvement of ex vivo permeation than free SV. The clinical study exhibited no comparable difference between F8 and marketed minoxidil lotion. However, F8 demonstrates less adverse effects than minoxidil lotion. Nanospanlastics could be a safe and effective method for improving the topical delivery of SV in the management of AGA.

Alpha Tocopherol Loaded in Liposome: Preparation, Optimization, Characterization and Sperm Motility Protection

Background: Alpha-tocopherol is a potent antioxidant involved in sperm protection particularly during cryopreservation. However, its poor solubility limits the optimal protection in aqueous solutions. Objective: The aim of this study was to enhance the solubility of α-tocopherol by the use of liposomes. Methods: The experimental approach consisted to load vitamin E in liposomes prepared by ethanol injection method and the optimization carried out by an experimental design. The optimum solution was characterized by high performance liquid chromatography and scanning electron microscope. Finely, the impact on sperm motility protection was studied by the freezing technic of bovine sperm. Results: The optimum solution was obtained when using 10.9 mg/ml of phospholipids, 1.7 mg/ml of cholesterol and 2 mg/ml of vitamin E. The liposome size was 99.86 nm, providing 78.47% of loaded efficiency. The results showed also a significant positive impact on sperm motility after hours of preservation. Conclusion: In conclusion, the current results showed the interest of liposome preparation as an alternative to enhance vitamin E solubility and to protect spermatozoa during cryopreservation.

Bulk and Microfluidic Synthesis of Stealth and Cationic Liposomes for Gene Delivery Applications.

This chapter describes the synthesis of stealth and cationic liposomes and their complexation with plasmid DNA to generate lipoplexes for gene delivery applications. Two techniques are presented: a top-down approach which requires a second step of processing for downsizing the liposomes (i.e., ethanol injection method) and a microfluidic technique that explores the diffusion of ethanol in water to allow the proper lipid self-assembly. The synthesis of stealth liposomes is also a challenge since the use of poly(ethylene glycol) favors the formation of oblate micelles. In this protocol, the stealth cationic liposome synthesis by exploring the high ionic strength to overcome the formation of secondary structures like micelles is described. Finally, the electrostatic complexation between cationic liposomes and DNA is described, indicating important aspects that guarantee the formation of uniform lipoplexes.

Preparation and Characterization of Ivabradine HCl Transfersomes for Enhanced Transdermal Delivery

Ivabradine HCl (IVB) is used in treatment of stable angina pectoris. The aim of the work was to prepare a once daily transdermal film of transfersomes loaded IVB. Transfersomes were prepared by modified ethanol injection method using three formulation factors namely: surfactant type, drug: phospholipid ratio and surfactant: phospholipid ratio. The transfersomes were characterized for entrapment efficiency, particle size, zeta potential, in vitro drug release, optical and transmission electron microscopy imaging, differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The best transfersomes showed optimal properties as well as pure drug were further formulated in transdermal film and characterized for content uniformity, folding endurance, weight and thickness, moisture content, moisture uptake, tensile strength and permeation through excised ear rabbit skin. Pharmacokinetic parameters of transfersomes incorporated film were compared with oral solution of the same drug dose. A maximum of about 82.03% entrapment efficiency, size of 206.7 nm, zeta potential of −88.3 Mv and 66.7% of drug release after 24 h were obtained from sodium lauryl sulphate based transfersomes at drug: phospholipid and surfactant: phospholipid ratio of 1:20 and 75:25 w/w, respectively. Films contained IVB transfersomes exhibited improved permeability and skin retention when compared with pure drug as well as enhanced pharmacokinetic parameters.

Preparation and In Vitro Characterization of Enoxaparin Nano-liposomes through Different Methods.

Purpose: Enoxaparin has been widely used as a choice drug for treatment and prevention of different coagulation disorders. Orally administered enoxaparin encounters with gastrointestinal barrier because of its high water solubility, high molecular weight and significant negative charge. Since, the nano-liposomes has gained great interest for oral drug delivery, we decided to introduce the best protocol for preparing enoxaparin nano-liposomes through in vitro characterization. Methods: Nano-liposomes were prepared by ethanol injection, thin film hydration, and double emulsion/solvent evaporation methods. Size distribution, zeta potential, loading efficiencies, and in vitro drug release of nano-liposomes were also studied. Results: The mean vesicle size was obtained under 100 nm, and the zeta potential was highly negative through all preparation methods. Nano-liposomes prepared by double emulsion/ solvent evaporation (DE) technique could entrap more of this hydrophilic drug (43 ± 7.1 %), but through thin layer hydration (TL) and ethanol injection (EI) only 28.4± 3.2% and 17.3 ± 2.5% of drug could be loaded into synthesized carriers. Drug release from these carriers was also obtained 42.17±1.72%, 29.43±0.34% and 32.27±0.14%, in 24 hours for EI, TL, and DE methods, respectively.Conclusion: Here, we can introduce double emulsion/solvent evaporation method as an acceptable method for enoxaparin loading, although some toxicity and in-vivo tests are also necessary to fully understand the potential of this formulation.

Development of cysteamine loaded liposomes in liquid and dried forms for improvement of cysteamine stability.

Despite the high aqueous solubility of cysteamine, its unpleasant organoleptic properties, hygroscopicity, instability in solutions, and poor pharmacokinetic profile are the main drawbacks that limit its use for medical and cosmetic purposes. In this study, cysteamine-loaded liposomes were prepared using the ethanol injection method. Liposomes were characterized for their size, homogeneity, surface charge, and morphology. The incorporation ratios of cholesterol and phospholipids, the encapsulation efficiency and the loading ratio of cysteamine in liposomes were determined. Moreover, the stability of free and encapsulated cysteamine was assessed at different temperatures (4, 25, and 37°C) in the presence and absence of light. Cysteamine-loaded liposomes were freeze-dried and reconstituted liposomes were characterized. Finally, the storage stability of the freeze-dried cysteamine-loaded liposomes was studied. Liposomes were nanometric, oligolamellar, and spherical. The encapsulation efficiency and the loading ratio of cysteamine varied between 12 and 40% in the different formulations. The encapsulation improved the stability of cysteamine in the various storage conditions. The dried form of cysteamine-loaded liposomes conserved the size of the vesicles and retained 33% of cysteamine present in the liposomal suspension before lyophilization. The freeze-dried liposomes formulations were stable after four months of storage at 4°C.

Optimization of Sterically stabilized liposome using design of experiment approach

Recently, a drug delivery system with controlled and targeted drug release at the tumor sites emerged as an attractive option for improving anticancer therapeutics. Advanced nanotherapeutics must not be limited to nanoscale, but should find their way to target the solid tumor via direct or indirect way. Pegylation on the surface of liposome helps to become liposome as long-circulating and indirect or passive targeting to tumors. The purpose of this study is to develop and optimize the critical process parameters, which play an important role in the quality pegylated liposome. The design of experiment (DoE) was used to study the impact of critical process variables like hydration temperature, extrusion process temperature, ethanol concentration, drug loading temperature, and drug loading time. Pegylated liposome was prepared using the ethanol injection method. Size reduction was achieved using the extrusion method. Drug encapsulation was achieved by a remote loading method using an ammonium phosphate gradient. A fractional factorial design was chosen for the optimization of process variables. Hydration temperature and extrusion process temperature directly impact on the degradation of lipids used in liposome formation. Higher temperature increases the lipid degradation during the process. The concentration of ethanol during the size reduction process inversely affects the particle size of the liposome. Higher the ethanol content lowers the particle size achieved. The temperature during drug loading process directly affects the degradation of the drug while inversely affect the encapsulation property. Stability study indicates that optimized formulation using DoE approach remains stable. The present research confirms the feasibility of developing and optimizing sterically stabilized liposome using DoE approach.

Co-encapsulation of Vitamin C and β-Carotene in liposomes: Storage stability, antioxidant activity, and in vitro gastrointestinal digestion

Vitamin C (VC) and β-Carotene (βC) were selected to produce co-encapsulated liposomes using hydrophilic and hydrophobic cavities simultaneously by ethanol injection method. The results of liposomal structure characterized by particle size, polydispersity index, zeta-potential and transmission electron microscope showed that the microstructure of all liposomal samples was spherical without adhesion or break and the size of VC-βC-loaded liposome (L-VC-βC) was bigger than VC-loaded liposome (L-VC) or βC-loaded liposome (L-βC). The encapsulation efficiency (EE) of VC in L-VC-βC was significantly higher than that in L-VC, and the EE of βC in L-VC-βC had no significant change compared with that in L-βC. The free radical scavenging rate of L-VC-βC was significantly higher than that of L-βC, while it had no significant change compared with that of L-VC. In addition, the storage stability of βC in L-VC-βC improved greatly compared with that in L-βC. Furthermore, the zero order model was applied to understand the release kinetics of βC from L-βC and L-VC-βC in the stomach, whereas the Korsmeyr-Peppas model was chosen to describe the release of βC from two types of liposome in small intestine and their release mechanisms were mainly dominated by Fickian diffusion. It was significant to provide a new idea for using hydrophilic and hydrophobic cavities simultaneously in liposomes to design the multicomponent nutrient delivery system.