High-pressure Homogenization Method Research Articles

Box-Behnken Design-Based Optimization and Evaluation of Lipid-Based Nano Drug Delivery System for Brain Targeting of Bromocriptine.

Bromocriptine (BCR) presents poor bioavailability when administered orally because of its low solubility and prolonged first-pass metabolism. This poses a significant challenge in its utilization as an effective treatment for managing Parkinson's disease (PD). The utilization of lipid nanoparticles can be a promising approach to overcome the limitations of BCR bioavailability. The aim of the research work was to develop and evaluate bromocriptine-loaded solid lipid nanoparticles (BCR-SLN) and bromocriptine-loaded nanostructured lipid carriers (BCR-NLC) employing the Box-Behnken design (BBD). BCR-SLNs and BCR-NLCs were developed using the high-pressure homogenization method. The prepared nanoparticles were characterized for particle size (PS), polydispersity index (PDI), and entrapment efficiency (EE). In vitro drug release, cytotoxicity studies, in vivo plasma pharmacokinetic, and brain distribution studies evaluated the optimized lipid nanoparticles. The optimized BCR-SLN had a PS of 219.21 ± 1.3 nm, PDI of 0.22 ± 0.02, and EE of 72.2 ± 0.5. The PS, PDI, and EE of optimized BCR-NLC formulation were found to be 182.87 ± 2.2, 0.16 ± 0.004, and 83.57 ± 1.8, respectively. The in vitro release profile of BCR-SLN and BCR-NLC showed a biphasic pattern, immediate release, and then trailed due to the sustained release. Furthermore, a pharmacokinetic study indicated that both the optimized BCR-SLN and BCR-NLC formulations improve the plasma and brain bioavailability of the drug compared to the BCR solution. Based on the research findings, it can be concluded that the BCR-loaded lipid nanoparticles could be a promising carrier by enhancing the BBB penetration of the drug and helping in the improvement of the bioavailability and therapeutic efficacy of BCR in the management of PD.

Zein/fucoidan-coated phytol nanoliposome: preparation, characterization, physicochemical stability, in vitro release, and antioxidant activity.

To improve phytol bioavailability, a novel method of magnetic stirring and high-pressure homogenization (HPH) combination was used to prepare zein/fucoidan-coated phytol nanoliposomes (P-NL-ZF). The characterization, the simulated in vitro digestion, and the antioxidant activity of these phytol nanoliposomes from the different processes have been studied. Based on the results of dynamic light scattering (DLS) and gas chromatography-mass spectrometer (GC-MS) analysis, P-NL-ZF prepared through the combination of magnetic stirring and HPH exhibited superior encapsulation efficiency at 76.19% and demonstrated exceptional physicochemical stability under a series of conditions, including storage, pH, and ionic in comparison to single method. It was further confirmed that P-NL-ZF by magnetic stirring and HPH displayed a uniform distribution and regular shape through transmission electron microscopy (TEM). Fourier-transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC) analysis showed that electrostatic interactions and hydrogen bonding were the primary driving forces for the formation of composite nanoliposomes. Additionally, an in vitro digestion study revealed that multilayer composite nanoliposomes displayed significant and favorable slow-release properties (58.21%) under gastrointestinal conditions compared with traditional nanoliposomes (82.36%) and free phytol (89.73%). The assessments of chemical and cell-based antioxidant activities demonstrated that the coating of zein/fucoidan on phytol nanoliposomes resulted in enhanced effectiveness in scavenging activity of ABTS free radical and hydroxyl radical and mitigating oxidative damage to HepG2 cells. Based on our studies, the promising delivery carrier of zein/fucoidan-coated nanoliposomes is contributed to the encapsulation of hydrophobic natural products and enhancement of their biological activity. © 2024 Society of Chemical Industry.

Physicochemical properties and antibacterial activity evaluation of new indigo extract from Baphicacanthus cusia (Nees) Bremek prepared by chemical conversion method

The effect of acidolysis time, hydrochloric acid concentration, ozonization time and pH on the yield of indigo were investigated by single factor experiment using dried leaves of Baphicacanthus cusia (Nees) Bremek (DLB) as raw material. On this basis, the technological condition for preparing new indigo extract (NIE) by directional chemical conversion method was optimized by orthogonal experiment. Then, the physiochemical properties of NIE were analyzed by combustion assay, nitric acid assay, thin layer chromatography identification assay, moisture detection and water-soluble pigment observation assay. Moreover, UPLC-Q-TOF-MS/MS technology was utilized to compare chemical composition difference between the NIE and traditional indigo naturalis (TIN). Finally, NIE emulsion was prepared by ultrasound assisted high pressure homogenization method and its stability, antibacterial activity as well as antibacterial mechanism were evaluated. The experimental results showed that optimum process for preparing NIE were hydrochloric acid concentration of 2 %, ozonization time of 3 min, pH of 7 and acidolysis time of 1 h; Under this condition, the content and yield of indigo in the NIE were significantly improved, which could reach up to 42.6 ± 0.28 % and 2.26 ± 0.04 %, separately. NIE possessed similar physiochemical properties with TIN described in Chinese pharmacopoeia 2020, and had more diverse active ingredients than TIN. The prepared NIE emulsion demonstrated excellent stability, whether at dark or bright place, and no matter at low temperature (4 ℃) or room temperature (25 ℃), the particle size, PDI, pH and indigo content of which displayed little variation. In addition, the NIE emulsion owned good inhibitory activity against S. aureus, and its MIC and MBC values were 40 and 80 μg/mL, respectively. Moreover, NIE emulsion exhibited antibacterial effect by influencing cell membrane integrity, Ca2+-Mg2+-ATPase activity on the cell membrane and intracellular Ca2+ levels of S. aureus. All of above results will lay the foundation for the green and sustainable utilization of Baphicacanthus cusia (Nees) Bremek.

Effects of solid lipid nanocarrier containing methyl urolithin A by coating folate-bound chitosan and evaluation of its anti-cancer activity

BackgroundNanotechnology-based drug delivery systems have received much attention over the past decade. In the present study, we synthesized Methyl Urolithin A-loaded solid lipid nanoparticles decorated with the folic acid-linked chitosan layer called MuSCF-NPs and investigated their effects on cancer cells.MethodsMuSCF-NPs were prepared using a high-pressure homogenization method and characterized using FTIR, FESEM, DLS, and zeta potential methods. Drug encapsulation was assessed by spectrophotometry and its cytotoxic effect on various cancer cells (MDA-MB231, MCF-7, PANC, AGS, and HepG2) by the MTT method. Antioxidant activity was assessed by the ABTS and DPPH methods, followed by expression of genes involved in oxidative stress and apoptosis by qPCR and flow cytometry.ResultsThe results showed the formation of monodisperse and stable round nanoparticles with a size of 84.8 nm. The drug loading efficiency in MuSCF-NPs was reported to be 88.6%. MuSCF-NPs exhibited selective cytotoxicity against MDA-MB231 cells (IC50 = 40 μg/mL). Molecular analysis showed a significant increase in the expression of Caspases 3, 8, and 9, indicating that apoptosis was occurring in the treated cells. Moreover, flow cytometry results showed that the treated cells were arrested in his SubG1 phase, confirming the pro-apoptotic effect of the nanoparticles. The results indicate a high antioxidant effect of the nanoparticles with IC50 values ​​of 45 μg/mL and 1500 μg/mL against ABTS and DPPH, respectively. The reduction of catalase gene expression confirmed the pro-oxidant effect of nanoparticles in cancer cells treated at concentrations of 20 and 40 μg/mL.ConclusionsTherefore, our findings suggest that the MuSCF-NPs are suitable candidates, especially for breast cancer preclinical studies.

Enhancement of hepatoprotective activity of limonin from citrus seeds against acetaminophen-induced liver injury by HSCCC purification and liposomal encapsulation

Limonin is a natural tetracyclic triterpenoid compound in citrus seeds that presents hepatoprotective effects but is often discarded as agricultural waste because of its low content and low solubility. Herein, limonin with high purity (98.11%) from citrus seeds was obtained via purification by high-speed counter-current chromatography (HSCCC) and recrystallization. Limonin-loaded liposomes (Lip-LM) prepared by thin film hydration and high pressure homogenization method to enhance its solubility and hepatoprotective effect on APAP-induced liver injury (AILI). Lip-LM appeared as lipid nanoparticles under a transmission electron microscope, and showed well dispersed nano-scale size (69.04 ± 0.42 nm), high encapsulation efficiency (93.67% ± 2.51%), sustained release, fine stability. Lip-LM also exhibited significantly better hepatoprotective activity on AILI than free limonin in vivo. In summary, Lip-LM might be used as a potential hepatoprotective agent in the form of dietary supplement and provide an effective strategy to improve the potential value of citrus seeds.

Nanocrystal-Loaded Lipid Carriers for Improved Oral Absorption and Anticancer Efficacy of Etoposide: Formulation Development, Transport Mechanism, In Vitro and In Vivo Evaluation.

To improve the oral absorption and anticancer efficacy of the BCS-IV drug etoposide (ETO), oral nanocrystal-loaded lipid carriers (Lipo@NCs) were developed in this study by modifying the BCS-IV drug nanocrystal with the lipid bilayer. The ETO-Lipo@NCs were prepared by the thin film hydration high-pressure homogenization method, and the core of positively charged ETO nanocrystals was prepared by the sonoprecipitation-high pressure homogenization method. The optimized ETO-Lipo@NCs were spherical particles with an average particle size of 220.3 ± 14.2 nm and a zeta potential of -9.95 ± 0.81 mV, respectively. The successful coating of a lipid bilayer on the surface of nanocrystals in ETO-Lipo@NCs was confirmed by several characterization methods. Compared to nanocrystals, the release rate and degree of Lipo@NCs in SIF were significantly decreased, indicating that the lipid bilayer can effectively prevent the rapid dissolution of core nanocrystals. ETO-Lipo@NCs demonstrated a significant improvement in the intestinal permeability and absorption of ETO in a single intestinal perfusion experiment. In the cells, ETO-Lipo@NCs showed enhanced cellular uptake and transepithelial transport compared with ETO nanocrystals. Pharmacokinetic analysis indicated that ETO-Lipo@NCs had a longer plasma half-life than ETO solution, and the oral bioavailability of ETO-Lipo@NCs was 1.96- and 10.92-fold higher than that of ETO nanocrystals and ETO coarse crystals, respectively. Moreover, the ETO-Lipo@NCs orally dosed at 10 mg/kg exhibited an excellent inhibitory effect against tumors in a subcutaneous Lewis lung carcinoma (LLC) xenograft model compared with other preparations. These results indicate that the Lipo@NCs formulation has an oral absorption-promoting effect of the BCS-IV drug ETO, which could warrant further application in the oral delivery of other poorly bioavailable drugs.

Remifentanil and Propofol Co-loaded Nanoemulsion: Formulation Development and In vivo Pharmacodynamic Evaluation

Background: The present work is an effort to develop novel propofol (PPF) and remifentanil (RFT) co-loaded nanoemulsion (NME) for the treatment of anesthetic effects. Methods: The PPF/RFT NME was prepared via the high-pressure homogenization method. Its physicochemical properties were assessed to ensure good quality and suitability for i.v. administration. We also studied the in vivo pharmacokinetics and pharmacodynamics of PPF/RFT NME in dogs with an optimized formulation. Results: This study showed that the mean particle size of PPF/RFT NME was 124.2 nm and the zeta potential was −20.6 mV. In the stability test, the NME maintained a good round shape and did not demonstrate any significant changes in physicochemical characteristics. In terms of the in vitro release, the early burst release of the NME preparations containing PPF or RFT was ideal in clinical practice, where a loading dose or a rapid onset of the drug was required. Based on histopathological observations, no histological change occurred to the rat organs after the administration of PPF/RFT NME. Regarding pharmacodynamics, compared with the combination group at the same dose, PPF/RFT NME could make animals enter the anesthetic state faster and the anesthetic effects last longer. In addition, vital signs of PPF/RFT NME could be maintained in a good state while better effects were delivered. Conclusions: This study used PPF and RFT to prepare a compound NME. This could reduce the anesthesiologist's administration time and make the anesthesia process more efficient.

Nanoemulsions: summary of a decade of research and recent advances.

Nanoemulsions consist of a combination of several components such as oil, water, emulsifiers, surfactants and cosurfactants. Various techniques for producing nanoemulsions include high-energy and low-energy approaches such as high-pressure homogenization, microfluidization, jet disperser and phase inversion methods. The properties of a formulation can be influenced by elements such as the composition, concentration, size and charge of droplets, which in turn can affect the technique of manufacture. Characterization is conducted by the assessment of several factors such as physical properties, pH analysis, viscosity measurement and refractive index determination. This article offers a thorough examination of the latest developments in nanoemulsion technology, with a focus on their wide-ranging applications and promising future possibilities. It also discusses the administration of nanoemulsions through several methods.

Unveiling the optimal path: High-pressure homogenization and D-phase emulsification methods for borage oil nanoemulsion design

Borage oil contains high levels of essential omega-6 fatty acids, which are important for skin structure and function. For this reason, this oil can be used for the treatment of cutaneous diseases including atopic dermatitis. This disease is associated with an abnormality in essential fatty acids (EFAs) metabolism, particularly in the production of gamma-linolenic acid, leading to impaired incorporation of EFAs into the phospholipid membrane. EFAs bioavailability can be enhanced by using a borage oil nano-based drug delivery system. In this study a borage oil nanoemulsion was prepared using high-pressure homogenization (HPH) and D-phase emulsification (DPE), respectively, high and low energy methods. A design space approach was performed to optimize the formulations. The optimized HPH nanoemulsion (HPH-NE) presented a particle size and zeta potential (ZP) of 425.3 ± 5.6 nm, and − 19.4 ± 3.7 mV, respectively. For the DPE nanoemulsion (DPE-NE) the particle size was 334.4 ± 5.2 nm, and the zeta potential was − 34.6 ± 1.0 mV. Furthermore, DPE-NE presented higher toxicity compared to HPH-NE, possibly related to the presence of the polyol. These nanoemulsions may improve the borage oil bioavailability for oral administration. Thus, they can be used as an adjuvant therapy in the treatment of atopic dermatitis.

Preparation of Piroxicam nanosuspensions by high pressure homogenization and evaluation of improved bioavailability

Objective Inflammation is a natural response of the organism, involving events responsible for releasing chemical mediators and requiring treatments of symptoms such as pain, redness, heat, swelling, and loss of tissue function. Piroxicam (PRX) is a non-steroidal anti-inflammatory drug with the effect of nonselective COX inhibitor activity; however, it shows poor bioavailability caused by the poor and slow water solubility. In this study, we developed PRX nanosuspensions with 200–500 nm in diameter to increase the bioavailability of PRX by improving its solubility. Methods PRX nanosuspensions were fabricated by High pressure homogenization method with PVA, SDS and Tween 80. The nanosuspensions were characterized by XRD, FTIR, DSC, and in vitro release. In vivo pharmacokinetic properties and anti-inflammatory effects were also investigated in rabbits. Results PRX nanosuspensions significantly increased the solubility (14.89 ± 0.03 mg/L for pure PRX and 16.75 ± 0.05 mg/L for PRX nanosuspensions) and dissolution rate as compared to the pure PRX (p < 0.05). Orally administered PRX nanosuspension (AUC 0-t is 49.26 ± 4.29 μg/mL × h) significantly improved the bioavailability of PRX (AUC 0-t is 28.40 ± 12.11 μg/mL × h). The anti-inflammatory effect of PRX nanosuspension was also investigated in rabbits and it was observed that PRX nanosuspension treatment significantly improved the inhibition of COX-2 and NFκB expression as compared to the PRX treatment (p < 0.05). Conclusions The results in this study indicate that PRX nanosuspension is a promising nanomedicine for enhancing the anti-inflammatory activity of PRX and has a high potential for the treatment of inflammation.

Assessing the In Vitro and In Vivo Performance of L-Carnitine-Loaded Nanoparticles in Combating Obesity.

Addressing obesity is a critical health concern of the century, necessitating urgent attention. L-carnitine (LC), an essential water-soluble compound, plays a pivotal role in lipid breakdown via β-oxidation and facilitates the transport of long-chain fatty acids across mitochondrial membranes. However, LC's high hydrophilicity poses challenges to its diffusion through bilayers, resulting in limited bioavailability, a short half-life, and a lack of storage within the body, mandating frequent dosing. In our research, we developed LC-loaded nanoparticle lipid carriers (LC-NLCs) using economically viable and tissue-localized nanostructured lipid carriers (NLCs) to address these limitations. Employing the central composite design model, we optimized the formulation, employing the high-pressure homogenization (HPH) method and incorporating Poloxamer® 407 (surfactant), Compritol® 888 ATO (solid lipid), and oleic acid (liquid oil). A comprehensive assessment of nanoparticle physical attributes was performed, and an open-field test (OFT) was conducted on rats. We employed immunofluorescence assays targeting CRP and PPAR-γ, along with an in vivo rat study utilizing an isolated fat cell line to assess adipogenesis. The optimal formulation, with an average size of 76.4 ± 3.4 nm, was selected due to its significant efficacy in activating the PPAR-γ pathway. Our findings from the OFT revealed noteworthy impacts of LC-NLC formulations (0.1 mg/mL and 0.2 mg/mL) on adipocyte cells, surpassing regular L-carnitine formulations' effects (0.1 mg/mL and 0.2 mg/mL) by 169.26% and 156.63%, respectively (p < 0.05).

Nanoencapsulation of crocin in double-layer emulsions for improved stability and enhanced efficacy against depression.

On average, depression affects 7.7% of the population aged 15 and older. One of the types of medicinal plants used to treat depression is saffron, which is uplifting and relieves sadness. Crocin as a bioactive compound is effective against depression, but it is sensitive to temperature, pH, and oxygen, and its efficiency decreases. Nanoencapsulation of crocin using double-layer emulsions is a method to increase the stability of this compound. Surfactant ratio (50% to 200%), stirrer speed (500 and 1000 rpm), and stirring time (45, 90, and 135 min) were used as variables of primary emulsion production. The optimum ratio of surfactant to aqueous phase was 100%, and in all microemulsions, viscosity increased with increasing surfactant ratio. A high-pressure homogenization method was used to make the secondary emulsion (double-layer emulsions), and soy protein concentrate (SPC), Gum Arabic (GA), and Pectin (P) at two levels of 5 and 10% were used to increase the stability. All treatments evaluated using Duncan's test at a significance level of 5%. Double-layer emulsions stabilized with pectin showed the highest viscosity and the lowest release of crocin in simulated stomach and intestine conditions. The use of the cellular automata model to investigate the release of crocin showed that this model could simulate the effects of crocin concentration, polymer concentration, and the droplet size of double-layer emulsions with 93-99% confidence to predict the release in double-layer emulsions. Then the double-layer emulsions added to the chocolate, and the chocolate containing the double-layer emulsions compared with the control sample in terms of sensory properties and had a higher score than the control sample.

Modification and Improvement of the Liposome Composition of Preputial Gland Extract of Siberian Musk Deer

In this work, we set out to characterize the liposomal form of a new original product based on the preputial gland extract of Siberian musk deer whose composition was modified by an inclusion complex with β-cy- clodextrin. Musk deer liposomes were obtained by an efficient and scalable high-pressure homogenization method. The resulting liposomal product was characterized by transmission electron microscopy, dynamic light scattering, preparative and analytical chromatography, and gas chromatography-mass spectrometry. A specification for the liposomal form of Siberian musk deer extract was developed, which includes all critical indicators of product quality. Homogeneous dispersions of musk deer liposomes with a uniform size distribution were obtained, with the distribution maxima observed at 50 and 240 nm. The high physicochemical stability of the liposomal dispersion was established with the zeta potential value of the obtained nanoparticles ranging from –5 to –35 mV. According to size-exclusion chromatography and mass spectrometry, the incorporation of deer musk target components into liposomes reached 58–75% for musk liposomes in terms of steroid components and total protein. The revealed quality indicators of the studied liposomal product indicate the possibility of obtaining highly effective products based on the liposomal form of musk deer extract, modified with cyclodextrin, as an adaptogen of natural origin with an enhanced and pronounced activity in laboratory performance tests.

Self-stabilizing performance of γ-oryzanol in oil-in-water emulsions and solid dispersions

The surface activity of γ-oryzanol was evaluated by the pendant drop method (PDM), and its self-stabilizing properties were investigated by high-pressure homogenization (HPH) and solvent displacement method (SDM). Emulsions prepared by HPH were highly unstable due to the poor surface-active character of γ-oryzanol as identified by the PDM. In contrast, solid dispersions fabricated by SDM had comparable particle size to those prepared using Tween 80 (T80) as surfactant, and were stable up to 30 days of storage at 4 °C. The self-stabilizing properties of γ-oryzanol were attributed to the mechanism of spontaneous particle formation in SDM and to the ability of γ-oryzanol molecules to prevent particles aggregation by electrostatic repulsion. The outcome of this study indicates the potential of encapsulating selected bioactive compounds, such as γ-oryzanol, in stable colloidal systems by SDM without adding emulsifier(s), regardless of their surface-active character.

Formulation and Evaluation of Simvastatin Nanoparticles

Present study was aimed to formulation and evaluation of Simvastatin nanoparticles. Simvastatin nanoparticles were prepared by High pressure homogenization method by using lipid (Glyceryl Monostearate), polymer (Chitosan, Sodium Alginate) and surfactant (Tween 80) in the formulation. The prepared nanoparticles were evaluated for particle size, zetapotential, entrapment efficiency, drug excipients compatability studies by FTIR, scanning electron microscopy and invitro release studies. Among all the formulations, The formulation F8 showed particle size 97.47nm, PDI as 0.333, zeta potential -30.60mV and % Entrapment efficiency 85.69%, FTIR studies shown that drug was compatable with excipients, Scanning electron microscopy results shown that particles in the formulation shows moderately spherical in shape and drug release maximum 97.28%. So, formulations F8 showed better sustain the drug release for 12hrs period of time as compared to other prepared formulations, hence drug release kinetics was applied for F8 formulation. Drug release kinetic studies it showed that optimized formulation F8 showed zero order with non-fickian mechanism.

Anti-obesity effects of chlorogenic acid and caffeine- lipid nanoparticles through PPAR-γ/C/EBP-ɑ pathways.

Obesity is considered one of the most crucial health problems of the century. Therefore, reducing obesity is critically important. Caffeine (CF) and chlorogenic acid (CLA), which are substantial components in green bean coffee which maximize thermogenesis in brown adipose tissue. In our study, we have prepared CF, CLA, and CF + CLA loaded-solid lipid nanoparticles (SLN) since the SLNs are cost-effective, tissue-localized, and highly stable. The central composite design model was preferred to select the optimized formulation. UHPLC was used for quantification related to the CF and CLA amounts. The high-pressure homogenization (HPH) method was used while SLN formulations were prepared in the presence of poloxamer® 407 (surfactant) and Compritol® 888 ATO (solid lipid). The nanoparticles were characterized, followed by the utilization of 3T3-F442A cell lines for the evaluation of the adipogenesis activity of the formulations. Then, rt-PCR and ELISA studies of adipogenic markers were conducted. After optimal formulations were selected with an average of 110.2 ± 0.1 nm, CF (1 mM) + CLA (0.5 mM)-loaded SLN formulation has been proven significantly effective by using PPAR-γ/C/EBP-a pathways. In a nutshell, our study has shown that CF + CLA loaded-SLN has been affected 45.8% times more than regular extracted coffee (p < 0.05) on the adipocyte cells.

Fabrication and functional attributes of nanotherapeutically engineered system for co-administration of adapalene and lycopene for enhanced acne management: an in vitro and in vivo investigation

BackgroundAcne vulgaris is caused due to several different biological, environmental and specific pathological factors, resulting in secretion of unregulated amount of sebum by the sebaceous glands. Acne is thought to be a minor, self-restraint, puberty leading and hormone-induced cosmetic disorder. It significantly affects the quality of life leading to social disengagement, anxiety, depression, necessitating its therapeutic management in due course of time. Thus, despite not being fatal it has social and mental impact on individual’s life. Pathogenesis of acne is complex and multifactorial involving diverse physiological, environmental factors and significant role of propionibacterium acne. Retinoids have been used as preferred first-line therapy for treatment of acne, but they have many limitations. Adapalene has found to be acting synergistically with other drugs like benzoyl peroxide, salicylic acid, clindamycin, etc., and various other topical antioxidants.ResultsThe study investigates the formulation and characterization of novel nanostructured lipid vesicles (NLVs) co-loaded with adapalene and lycopene, through topical gel. The high-pressure homogenization method was used to prepare nanostructured lipid vesicles followed by incorporation into hydrophilic gel vehicle. This novel system was scientifically tested for various evaluation parameters like size and vesicle size distribution, polydispersity index, drug entrapment efficiency and in vitro drug release characteristics, along with rheological behavior of formulation gel. Skin permeation and biodistribution characteristics through skin were also evaluated, and better localization of drug in dermis and reduced systemic penetration were the key observation in prepared formulation.ConclusionThe simultaneous co-administration of lycopene resulted in an additive effect in therapeutic management of acne. It can be predicted that this novel NLVs-based gel along with synergistic effect of lycopene will definitely result in better therapeutic efficacy and reduced systemic adverse effects of adapalene. This combination can be explored as future alternative for acne therapy.

Ethosome Containing Ceramide as a Skin Carrier of Active Ingredients.

Numerous formulations have been utilized in the cosmetic and pharmaceutical industries to effectively deliver bioactive ingredients. We selected a well-known liposomal formulation of bilayer lipid vesicles composed of ceramide NP. Ethosomes contain hydrophilic vanillic acid or lipophilic α-bisabolol, and their physicochemical properties were evaluated. Vanillic acid is encapsulated in the aqueous core while α-bisabolol is engaged with the lipid phase. The formulation was prepared by the high-pressure homogenization method at 800 bar for 5 min. The particle size, polydispersity index and zeta potential of the ethosome dispersion were analyzed by dynamic light scattering. In order to measure the skin absorption efficiency from artificial skin, an in vitro assay was performed using the Franz diffusion cell method for 24 hours. In addition, ultracentrifuges for encapsulation efficiency, dialysis membranes for active ingredient release, and low-temperature transmission electron microscopy (TEM) to evaluate the morphology of vesicles were utilized. The particle size of the ethosome containing ceramide NP and vanillic acid was in the range of 80 ~ 130 nm, whereas the particle size of the ethosome containing ceramide NP and α-bisabolol was 150 ~ 170 nm. In the vanillic acid-containing ethosome, increasing the amount of ceramide NP decreased the particle size, whereas the size of the α-bisabolol ethosome did not change. The stability of the prepared ethosome did not change significantly for 4 weeks at 25°C, 4°C, and 45°C. The skin absorption efficiency of ceramide NP and vanillic acid-containing ethosome was increased by about 15% compared to the control group, whereas the ethosome containing α-bisabolol and ceramide NP showed slightly higher skin absorption efficiency than the control group. In addition, encapsulation efficiency evaluation, active ingredient release measurement and cryo-TEM were taken. Based on the results of these studies, we suggest that ethosome formulations containing ceramide NP can be widely used in the cosmetic industry together with other cosmetic formulations.

Liposome-assisted penetration and antiaging effects of collagen in a 3D skin model.

Collagen is a major component of the extracellular matrix that supports the epidermal layers of the skin; thus, many strategies have been made to enhance the topical delivery of collagen for antiaging purposes. In addition, our previous study indicated that liposome can help the penetration of active ingredients into the skin. To produce stable collagen-encapsulated liposomes to improve the topical delivery of collagen. Collagen-encapsulated liposomes were fabricated using high-pressure homogenization method. The colloidal stability and adhesion ability were confirmed using dynamic light scattering, and spectrofluorophotometer, respectively. Keratinocyte differentiations of 3D skin before and after treatment with collagen-encapsulated liposomes were confirmed by real-time PCR. In comparison with native collagen, collagen-encapsulated liposomes enhanced collagen retention in artificial membranes by twofold, even after repeated washings with water. In addition, real-time PCR results indicated that 3D skin treated with collagen-encapsulated liposomes exhibited higher levels of collagen, keratin, and involucrin, even after ethanol treatment. Liposomes could serve as efficient delivery vehicles for collagen, thereby enhancing its antiaging effects.

Nano-crystals a comprehensive review on formulation and application perspectives

A majority of recently invented medications have been discovered to be poorly water-soluble and cause delays in the formulation and development of dosage forms. Solubility has been a major problem for BCS classes II and IV. As a result, nanotechnology may be useful in resolving the solubility problem. This review will cover Nanocrystals, as well as the numerous methodologies employed in their formulation and their application. Nanocrystals are nanometre-sized drug particles of a poorly water-soluble compound. They are distinct from polymeric nanoparticles in that they are entirely made up of the drug. Nanocrystals can be implemented to increase the rate of dissolution and saturation solubility of active pharmaceutical ingredients. Milling, high-pressure homogenization, precipitation, and combination methods such as Nanoedge andSmartCrystal, are among the approaches available for its formulation. The transition of nanocrystals into final formulations, as well as future nanocrystal trends, are also discussed.