Fabrication of a uniformly sized fenofibrate microemulsion by membrane emulsification

Fenofibrate-loaded microemulsions composed of Labrafil M 1944 CS, Capryol PGMC and fenofibrate as the dispersed phase and Labrasol in demineralised water as the continuous phase were prepared by utilising a Shirasu-porous-glass (SPG) membrane emulsification technique. The process parameters were optimised by adjusting the feed pressure (15–45?kPa), agitator speed (250–800?rpm) and temperature of the continuous phase (25–45°C). As a result, narrowly distributed microemulsions were obtained via SPG membrane emulsification at an agitator speed of 250?rpm, a feed pressure of 30?kPa and a continuous phase temperature of 25°C. Furthermore, TEM images clearly showed that the microemulsion prepared by SPG membrane emulsification had a uniform, spherical morphology with a narrow size distribution. Our results indicated that the SPG membrane emulsification technique is highly efficient for the preparation of narrowly distributed microemulsions with relatively smaller particle sizes compared with the common stirring method.     

Enhanced solubility and oral bioavailability of itraconazole by combining membrane emulsification and spray drying technique

The objective of the present study was to enhance solubility and bioavailability of itraconazole by a combined use of membrane emulsification and spray drying solidification technique. A shirasu-porous-glass (SPG) membrane with a mean pore size of 2.5 μm was used to produce monodispersed microemulsions of itraconazole consisting of methylene chloride as the dispersed phase, a mixture of Transcutol HP and Span 20 as a stabilizer, and dextran as solid carrier dissolved in water as the continuous phase. The dispersed phase permeated through the SPG membrane into the continuous phase at an agitator speed of 150 rpm, a feed pressure of 15 kPa and a continuous phase temperature of 25°C and the resultant emulsion was solidified using spray-drying technique. Solid state characterizations of the solid emulsion showed that the crystal state of itraconazole in solid emulsion was converted from crystalline to amorphous form. The solid emulsion of itraconazole displayed a significant increase in the dissolution rate than that of pure itraconazole. Furthermore, the solid emulsion after oral administration gave about eight-fold higher AUC and about ten-fold higher C(max) in rats than pure itraconazole powder (p<0.05), indicating this formulation greatly improved the oral bioavailability of drug in rats. Thus, these results demonstrated that the SPG membrane emulsification system combined with spray-drying technique could be used as a promising technique to develop solid formulation of itraconazole with enhanced solubility and bioavailability.     

Microencapsulation of menthol by crosslinked chitosan via porous glass membrane emulsification technique and their controlled release properties

Chitosan-encapsulated menthol microcapsules were successfully prepared in an oil-in-water (o/w) emulsion using the Shirasu Porous Glass (SPG) membrane emulsification technique and high-speed dispersion technique for preparing a mixed o/w emulsion. The size of the menthol-loaded chitosan microcapsules was strongly depended on the average pore size of the SPG membrane and the amount of menthol loading in the dispersed phase. The membrane pore size of 5.2?µm was suitable for a viscous dispersed phase containing light mineral oil. The average diameter of emulsion droplets of 28.3?µm was obtained. Increasing the menthol loading in the dispersion phase from 5% to 10% w/w of chitosan decreased the emulsion droplet size with a broad size distribution. The crosslinked microcapsule size and size distribution of mixed emulsion droplets decreased with the increasing crosslinking time. The menthol release was a diffusion control which depended on the proportion of amino group in chitosan-to-tripolyphosphate molar ratio and crosslinking time. This work also demonstrated that hydrophilicity/hydrophobicity of the continuous phase and dispersion phase controlled SPG membrane emulsification efficiency and quality of the resulting emulsion droplets.     

Study of the emulsion‐diffusion of solvent: preparation and characterization of nanocapsules

The objective of this work was to obtained stable nanocapsules (NC), that is to say a core shell structure by a recently patented method, the emulsion diffusion of solvent. To study the capacity of encapsulation, the aim was first to control the nanocapsules size distribution before the characterization of the membrane. Nanocapsules (NC) were prepared by an emulsion‐diffusion method. The emulsion was prepared using a high‐speed stirrer (Ultraturrax T25), and the droplet size distributions were determined. The mechanism of particle formation is based on the diffusion of the solvent followed by the deposition of the polymer around the oil droplet. The solvent partially soluble in the water and included in oil droplets diffuses into the outer aqueous medium after the emulsion dilution with water. It is then removed under reduced pressure. In order to control the NC sizes, we studied the effect of various emulsion parameters such as the nature and the concentration of the polymer, the stabilizer, the organic/aqueous phases ratio on NC morphology and size. The mean size of NC was about 500 nm, but we could have NC with diameter size between 200 to 1,000 nm. Size distributions were found to be function of the polymer/oil ratio in the organic phase, and of the solvent volume in the droplet. The suspension of nanocapsules were characterized by Transmission Electron Microscopy (TEM), Nuclear Magnetic Resonance (NMR), density gradient centrifugation, and Differential Scanning Calorimetry (DSC). The formation of nanocapsules involves mass transfer of solvent, polymer, and oil between phases. The physicochemical properties of the system can be classified into transport parameters such as solvent diffusion into the non‐solvent and interaction parameters such as solvent solubility in the water and the polymer. The mechanism of NC formation was investigated experimentally by monitoring the solvent concentration as a function of time in the continuous phase after different dilutions. The solvent elimination in the NC was complete after a dilution step followed by an evaporation under reduced pressure. This NC study gave some important information on their structure (core shell). The mechanism of formation based on the diffusion of solvent towards the aqueous phase was very rapid and depended on the volume of water at a kinetic level. We also showed that the state of the polymer changes and that the polymer forms the shell around the oil. Drug Dev. Res. 57:18–33, 2002. © 2002 Wiley‐Liss, Inc.     

The development and characterisation of triglyceride-based 'spontaneous' multiple emulsions

The formation of multiple emulsion droplets from two oil systems (Labrafil M 1944 CS and Labrafac Lipophile WL 1349) via a one-step process involving minimal agitation in aqueous media has been investigated in terms of the multiple character of the droplets, the particle size distribution, the stability and the lipolysis profile in the presence of pancreatic lipase. It was noted that multiple emulsion droplets were formed from both oils in the presence and absence of Tween 80, with the stability and particle size of the droplets being dependent on the composition and choice of media. It was noted that optimum stability of up to several days was obtained using 10% Tween 80 for both oils, with two stages of the breakdown process being apparent, the relative propensities of which being dependent on the oil used. The particle size distribution in distilled water indicated the presence of two distinct size populations corresponding to multiple and single droplets. It was noted that droplet breakdown was greatly accelerated in simulated intestinal fluid and in high pH media, with evidence for liquid crystal structure formation apparent. Lipolysis studies indicated that pegylation and the presence of surfactant slowed the degradation process. The study has indicated that ‘spontaneous’ multiple emulsion formation is indeed possible, with a reasonable if not necessarily optimal stability profile being observed for these systems.     

Effervescent atomization of aqueous polymer solutions and dispersions.

The purpose of this paper is to characterize the performance of effervescent atomizers via the effects of Air-to-Liquid-Mass-Ratio, (ALMR), feed pressure, and liquid viscosity on spray droplet size. Water and aqueous solutions having varying concentrations of polyvinylpyrrolidone, (PVP), (Kollidon 30, 90, and the copolymer VA 64), hydroxypropyl methylcellulose, (HPMC), (Pharmacoat 603, 606, and 615), and aqueous polymethacrylate dispersions, (Eudragit RS 30 D, RL 30 D, and L 30 D-55) were sprayed over a range of ALMRs from approximately 0.1 to 0.8 at feed pressures ranging from approximately 550 to 1590 kPa. Fluid viscosities ranged from 1 to 228 mPa.s. The ALMR of the spray was shown to be the most important factor influencing the Sauter mean diameter (SMD) of the droplets, while feed pressure was shown to have only a minor effect on droplet size. Sprays with SMDs between 7 and 12 microns were produced for the polymethacrylates, 13 to 24 microns for the PVPs, and 15 to 20 microns for the HPMCs, all at an ALMR of 0.4 and a feed pressure of 1172 kPa. A higher liquid viscosity lead to larger droplets. The correlation between viscosity and droplet size was found to be dependent on the type of polymer.     

Rheology and stability of water-in-oil-in-water multiple emulsions containing Span 83 and Tween 80

Multiple emulsions are often stabilized using a combination of hydrophilic and hydrophobic surfactants. The ratio of these surfactants is important in achieving stable multiple emulsions. The objective of this study was to evaluate the long-term stability of water-in-oil-in-water (W/O/W) multiple emulsions with respect to the concentrations of Span 83 and Tween 80. In addition, the effect of surfactant and electrolyte concentration on emulsion bulk rheological properties was investigated. Light microscopy, creaming volume, and rheological properties were used to assess emulsion stability. It was observed that the optimal surfactant concentrations for W/O/W emulsion long-term stability were 20% wt/vol Span 83 in the oil phase and 0.1% wt/vol Tween 80 in the continuous phase. Higher concentrations of Tween 80 had a destructive effect on W/O/W emulsion stability, which correlated with the observation that interfacial film strength at the oil/water interface decreased as the Tween 80 concentration increased. High Span 83 concentrations increased the storage modulus G′ (solidlike) values and hence enhanced multiple emulsion stability. However, when 30% wt/vol Span 83 was incorporated, the viscosity of the primary W/O emulsion increased considerably and the emulsion droplets lost their shape. Salt added to the inner aqueous phase exerted an osmotic pressure that caused diffusion of water into the inner aqueous phase and increased W/O/W emulsion viscosity through an increase in the volume fraction of the primary W/O emulsion. This type of viscosity increase imposed a destabilizing effect because of the likelihood of rupture of the inner and multiple droplets.     

Flurbiprofen-loaded nanoparticles prepared with polyvinylpyrrolidone using Shirasu porous glass membranes and a spray-drying technique: nano-sized formation and improved bioavailability

A unique flurbiprofen-loaded nanoemulsion was listed earlier using a Shirasu porous glass (SPG) membrane emulsification technique, which gave constant emulsion droplets with a thin size distribution. In this study, a flurbiprofen-loaded nanoemulsion was developed further into a solid form using polyvinylpyrrolidone (PVP) as a carrier by a spray-drying technique. The flurbiprofen-loaded nanoparticles with a weight ratio of flurbiprofen/PVP/surfactant mixture of 1/8/2 were connected with about 130?000-fold enhanced drug solubility and had a mean size of about 70?nm. In these nanoparticles, flurbiprofen was found in an altered amorphous state. Additionally, the nanoparticles gave significantly shorter T_max, and greater AUC and C_max compared to the commercially available product. Specially, the AUC of the drug from the nanoparticles was about 10-fold greater compared to the commercially available product. Therefore, these flurbiprofen-loaded nanoparticles can be convenient for distributing a poorly water-soluble flurbiprofen with improved bioavailability using uniform nano-sized particles.     

Effervescent Atomization of Aqueous Polymer Solutions and Dispersions

The purpose of this paper is to characterize the performance of effervescent atomizers via the effects of Air-to-Liquid-Mass-Ratio, (ALMR), feed pressure, and liquid viscosity on spray droplet size. Water and aqueous solutions having varying concentrations of polyvinylpyrrolidone, (PVP), (Kollidon® 30, 90, and the copolymer VA 64), hydroxypropyl methylcellulose, (HPMC), (Pharmacoat® 603, 606, and 615), and aqueous polymethacrylate dispersions, (Eudragit® RS 30 D, RL 30 D, and L 30 D-55) were sprayed over a range of ALMRs from approximately 0.1 to 0.8 at feed pressures ranging from approximately 550 to 1590 kPa. Fluid viscosities ranged from 1 to 228 mPa.s. The ALMR of the spray was shown to be the most important factor influencing the Sauter mean diameter (SMD) of the droplets, while feed pressure was shown to have only a minor effect on droplet size. Sprays with SMDs between 7 and 12 μm were produced for the polymethacrylates, 13 to 24 μm for the PVPs, and 15 to 20 μm for the HPMCs, all at an ALMR of 0.4 and a feed pressure of 1172 kPa. A higher liquid viscosity lead to larger droplets. The correlation between viscosity and droplet size was found to be dependent on the type of polymer.     

不同方法制备枸杞籽油微乳的比较研究

目的:优选枸杞籽油微乳的处方组成,比较枸杞籽油微乳的3种制备方法。方法:以枸杞籽油自身作为油相,利用外观、乳滴粒径、三元相图和伪三元相图等评价指标,优选枸杞籽油微乳的制剂处方;以乳滴粒径和粒度分布为指标,比较超声乳化法、高压乳匀法和自乳化法制备枸杞籽油微乳的不同特点。结果:优选的处方为1%枸杞籽油、1%吐温80、2%甘油;超声乳化法的工艺参数为超声功率480W,工作-间歇时间为10s-5s,超声时间25min,制得微乳的平均粒径为(74.6±45.3)nm(多分散系数(P.I)=0.368);高压乳匀法的工艺参数为均质压力500bar循环3次,制得微乳平均粒径为(69.0±31.5)nm(P.I=0.378);在相同处方比例下,自乳化法无法自发形成微乳,而当枸杞籽油:吐温80:甘油=1:7:2时,可自发形成微乳。结论:不同方法均能制得粒径小而均匀、外观透明有乳光的枸杞籽油微乳,但各法适用范围和特点不同。     

Characteristics of felodipine-located poly(epsilon-caprolactone) microspheres

Felodipine-loaded poly (epsilon-caprolactone) (PCL) microspheres were prepared by two methods, the conventional emulsion solvent evapouration method and the quenching method. The aim of this work was to investigate the effects of process parameters such as emulsion type, drug loading, molecular-weight of the polymer, types of emulsion stabilizer and dispersed phase solvents, as well as preparation methods. The results show that, when conventional emulsion solvent evapouration method was used, the o/w-method produced smaller mean size and higher encapsulation efficiency compared with the o/o-method. The encapsulation efficiencies increased with an increase in the molecular weight and a decrease in crystallinity of PCL. The size of microspheres varied with the type of emulsion stabilizer used, smaller microspheres with PVA and narrow size distribution with Pol 237. The water solubility of the dispersed phase solvent was one of the critical factors in controlling the encapsulation efficiency and microsphere mean size. When water-soluble solvents such as acetonitrile and ethyl formate were used, the encapsulation efficiencies decreased due to higher evapouration rate. When quenching methods were used, in contrast to the conventional emulsion solvent evapouration method, very narrowly size-distributed but bigger microspheres were obtained.     

Nanoemulsion system for the transdermal delivery of a poorly soluble cardiovascular drug

The purpose of the present study is to develop and evaluate the potential of nanoemulsions for increasing the solubility and the in vitro transdermal delivery of carvedilol. Pseudoternary phase diagrams were developed and various nanoemulsion formulations were prepared using oleic acid and isopropyl myristate (IPM) (1:1) as the oil, Tween 80 as surfactant, and Transcutol P as cosurfactant. The prepared nanoemulsions were subjected to physical stability tests. Transdermal permeation of carvedilol through rat abdominal skin was determined with Keshary-Chien diffusion cell. Significant increase (P < 0.05) in the steady state flux (Jss) and permeability coefficient (Kp) was observed in nanoemulsion formulations as compared to control or drug-loaded neat components. The highest value of these permeability parameters was obtained in optimized formulation B3, which consisted of 0.5% w/w of carvedilol, 6% w/w of oleic acid:IPM (1:1), 22.5% w/w of Tween 80, 22.5% w/w of Transcutol P, and 49% w/w of distilled water and in which the solubility of the drug was 4500-fold higher. The optimized nanoemulsion was characterized for pH, conductivity, viscosity, droplet size, droplet shape, and refractive index. Thermodynamic studies showed that there had been a significant decrease of 88% in activation energy (Eact) when the drug was incorporated in nanoemulsion. The irritation studies suggested that the optimized nanoemulsion was a non-irritant transdermal delivery system.     

Characteristics of felodipine-located poly(ε-caprolactone) microspheres

Felodipine-loaded poly (ε-caprolactone) (PCL) microspheres were prepared by two methods, the conventional emulsion solvent evapouration method and the quenching method. The aim of this work was to investigate the effects of process parameters such as emulsion type, drug loading, molecular-weight of the polymer, types of emulsion stabilizer and dispersed phase solvents, as well as preparation methods. The results show that, when conventional emulsion solvent evapouration method was used, the o/w-method produced smaller mean size and higher encapsulation efficiency compared with the o/o-method. The encapsulation efficiencies increased with an increase in the molecular weight and a decrease in crystallinity of PCL. The size of microspheres varied with the type of emulsion stabilizer used, smaller microspheres with PVA and narrow size distribution with Pol 237. The water solubility of the dispersed phase solvent was one of the critical factors in controlling the encapsulation efficiency and microsphere mean size. When water-soluble solvents such as acetonitrile and ethyl formate were used, the encapsulation efficiencies decreased due to higher evapouration rate. When quenching methods were used, in contrast to the conventional emulsion solvent evapouration method, very narrowly size-distributed but bigger microspheres were obtained.     

An improvement of double emulsion technique for preparing bovine serum albumin-loaded PLGA microspheres

A modified double emulsion technique was adopted to prepare bovine serum albumin (BSA) loaded poly (D,L-lactic-co-glycolic acid) (PLGA) microspheres. In the formulations, polysorbates (Tween) such as Tween20, Tween40 or Tween80, instead of frequently used poly (vinyl alcohol) (PVA), was used as the emulsifier. Microspheres with porous surface, large particle size, low microsphere yield (approximately 65.4%) and BSA entrapment efficiency (approximately 25.2%) were obtained when Tween80 aqueous solution alone was used as the outer aqueous phase. However, microspheres with smooth surface, high yield and BSA entrapment efficiency could be produced successfully by introducing sodium chloride or glucose into the outer aqueous phase. Adding 5.0%(w/v) sodium chloride into the continuous phase led to increase in microsphere yield and BSA entrapment efficiency from 65.4% and 25.2% to approximately 100% and 76.6%, respectively. Microsphere yield and BSA entrapment efficiency increased from 64.5% and 25.2% to 97.2% and 89.3%, respectively, when 15.0%,(w/v) glucose was added into the continuous phase. In constrast to the microspheres prepared in the presence of additive, a more marked burst release was observed for microspheres prepared without additive in the continuous phase, which may be attributed to the porous morphology of the latter.     

Polysaccharide-coated oil droplets in oil-in-water emulsions as targetable carriers for lipophilic drugs

Surface of oil droplets in an oil-in-water (o/w) emulsion were coated with naturally occurring polysaccharides (such as mannan, amylopectin, and pullulan) which were, in part, bearing a cholesterol moiety. The mean size of the colloidal droplets was not altered much, even by coating with the polysaccharide derivatives, while the surface charge of the droplet decreased upon coating. Mannan and amylopectin derivative-coated droplets aggregated upon addition of Concanavalin A. These observations suggest that the terminal sugar moiety of the specific polysaccharides on the surface of colloidal droplets can be recognized by lectin. After intravenous injection of the emulsions into guinea pigs, kinetics of the blood clearance and the tissue distribution of the polysaccharide-coated oil droplets, which contain [14C]coenzyme Q10 as the marker, were investigated. In the initial rapid phase of blood clearance of the radioactivity, the polysaccharide-coated droplets were cleared from the blood stream slower than the uncoated ones. The lung uptake of the mannan derivative-coated droplet emulsion at 30 min after intravenous injection was approximately 15 times higher than that of the conventional emulsion without the polysaccharide coat.     

Preparation and characterization of flurbiprofen-loaded poly(3-hydroxybutyrate-co-3-hydroxyvalerate) microspheres

Poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) microspheres containing flurbiprofen were prepared by an oil-in-water emulsion solvent evaporation method, in order to develop a particulate drug delivery system for localized administration. A response surface method (RSM) using a central composite design was employed to evaluate the effect of the poly(vinyl alcohol) (PVA) (%, w/v) concentration in the aqueous phase and the PHBV concentration in the organic phase (%, w/v) on some of the resulting microspheres properties. The response variables were the encapsulation efficiency (EE), the mean particle size, the width of particle size distribution (expressed by the SPAN value) and the required time for the in vitro release of 50% of the encapsulated drug (t(50%)). Second-order polynomial and linear equations were fitted to experimental data and were also used to interpret the results. Results indicated that the concentration of the stabilizer (PVA) showed a highly negative effect on the EE probably due to the increased drug solubility in the aqueous phase as a result of the higher PVA concentrations. Particle diameter mean size increased with the increased polymer concentration while the width of the particle size distribution was found to decrease with the increase of the stabilizer agent. Finally, results indicated that none of the investigated variables presented a significant effect on the t(50%) values.     

An improvement of double emulsion technique for preparing bovine serum albumin-loaded PLGA microspheres

A modified double emulsion technique was adopted to prepare bovine serum albumin (BSA) loaded poly (D,l-lactic-co-glycolic acid) (PLGA) microspheres. In the formulations, polysorbates (Tween) such as Tween20®, Tween40® or Tween80®, instead of frequently used poly (vinyl alcohol) (PVA), was used as the emulsifier. Microspheres with porous surface, large particle size, low microsphere yield (～65.4%) and BSA entrapment efficiency (～25.2%) were obtained when Tween80® aqueous solution alone was used as the outer aqueous phase. However, microspheres with smooth surface, high yield and BSA entrapment efficiency could be produced successfully by introducing sodium chloride or glucose into the outer aqueous phase. Adding 5.0%(w/v) sodium chloride into the continuous phase led to increase in microsphere yield and BSA entrapment efficiency from 65.4% and 25.2% to ～100% and 76.6%, respectively. Microsphere yield and BSA entrapment efficiency increased from 64.5% and 25.2% to 97.2% and 89.3%, respectively, when 15.0%(w/v) glucose was added into the continuous phase. In constrast to the microspheres prepared in the presence of additive, a more marked burst release was observed for microspheres prepared without additive in the continuous phase, which may be attributed to the porous morphology of the latter.     

内水相添加氯化钠对W/O/W型复乳性质的影响

目的探讨在内水相中添加氯化钠(NaCl)对W/O/W型复乳性质的影响。方法在前期试验优选出较佳W/O/W复乳处方的基础上,以1 g/L NaCl水溶液代替处方中的纯化水作为内水相,采用二步乳化法制备复乳,从显微结构、粒径分布、稳定性等方面比较复乳性质的变化。结果在内水相中添加NaCl(1 g/L)时,复乳主要为B型结构,外观较圆整,液滴大小较均匀,且乳滴不易聚集成一团,大部分粒子粒径在20～40μm之间,稳定性良好。结论在内水相中添加NaCl(1 g/L),有助于优化W/O/W型复乳物理化学性质,提高其稳定性。     

Correlation of physical parameters of an oil in water emulsion with manufacturing procedures and stability

The effect of nine process variables for the manufacture of a semi solid paraffin-in-water emulsion prepared with two nonionic surfactants, steareth 21 and sorbitan oleate were examined initially and following ageing for 2 and 4 years. The techniques employed included differential scanning calorimetry (DSC), small angle X-ray diffraction (SAXD) and microscope (differential interference contrast (DIC) and crossed polars). A previous paper (Lashmar, Int. J. Pharm., (1993) 59–67) used particle size analysis and theological techniques to evaluate the emulsions. It was concluded that the total DSC enthalpy change was an important indicator of the stability of an oil-in-water emulsion and that the appearance of a sample under crossed polars could be used as a guide. SAXD was not found to be suitable for evaluation of process parameters. The thermal properties of the emulsions and their appearance under crossed polars suggested that the homogenisation speed of the manufacturing vessel probably was the single most important factor for the production of a stable emulsion and that extending the homogenisation time would improve the stability of the emulsion. Cooling the emulsion slowly appeared to benefit its stability, whereas the speed at which the water phase was added to the oily phase during the emulsification process, the emulsification temperature and the speed of the agitator during cooling seemed to have little effect on the stability of the emulsion. Adding the surfactants to the aqueous phase before emulsification and adding the oil phase to the water phase during the emulsification produced inferior emulsions. On cooling, the optimum stability was achieved when the agitator was stopped around the temperature corresponding to the lower cooling exotherm for the sample. Results from this and the previous paper (Lashmar, 1993) indicated that the droplet size and the rheological properties could be manipulated by process parameters without affecting the stability of the product. A later paper will investigate other techniques to evaluate emulsions and manufacturing parameters.     

Fabrication,in-vitro characterization,and enhanced in-vivo evaluation of carbopol-based nanoemulsion gel of apigenin for UV-induced skin carcinoma

The aim of this study was to develop a potential novel formulation of carbopol-based nanoemulsion gel containing apigenin using tamarind gum emulsifier which was having the smallest droplet size, the highest drug content, and a good physical stability for Skin delivery. Apigenin loaded nanoemulsion was prepared by high speed homogenization method and they were characterized with respect to morphology, zeta potential, differential scanning calorimeter study, and penetration studies. In-vitro release studies and skin permeation of apigenin loaded nanoemulsion by goat abdominal skin was determined using Franz diffusion cell and confocal laser scanning microscope (CLSM). The cytotoxicity of the reported formulation was evaluated in HaCaT Cells (A) and A431 cells (B) by MTT assay. The nanoemulsion formulation showed droplet size, polydispersity index, and zeta potential of 183.31?nm, 0.532, and 31.9?mV, respectively. The nanoemulsions were characterized by TEM demonstrated spherical droplets and FTIR to ensure the compatibility among its ingredients. CLSM showed uniform fluorescence intensity across the entire depth of skin in nanocarriers treatment, indicating high penetrability of nanoemulsion gel through goatskin. The nanoemulsion gel showed toxicity on melanoma (A341) in a concentration range of 0.4–2.0?mg/ml, but less toxicity toward HaCaT cells. The carbopol-based nanoemulsion gel formulation of apigenin possesses better penetrability across goatskin as compared to marketed formulation. Hence, the study postulates that the novel nanoemulsion gel of apigenin can be proved fruitful for the treatment of skin cancer in near future.