Hot High Pressure Homogenization Technique Research Articles

Blending Ethnomedicine with Modern Technology-From Conventional to Tailored Products: Modulating Biopharmaceutical Properties of Berberis Extract by Solid Lipid Nanoparticles for Wound Healing.

Drug-delivery systems employing phytopharmaceuticals based on the leads in traditional knowledge offers not only an alternative but quicker and more economic strategy for drug development. Nanophytopharmaceuticals promise remarkable opportunities with the ability to overcome challenges associated with herbal medicines, such as low solubility and bioavailability, poor target specificity, and shelf life. Berberis extracts documented as Ropana (wound healer) in Sushruta Samhita are a popular traditional remedy that is amiss in the modern system of medicine as it exhibits very poor biopharmaceutical properties. Poor solubility and bioavailability necessitate the administration of high doses to achieve the desired therapeutic effects. Exploiting the diversified type of compounds with pleiotropic properties present in Berberis, the biopharmaceutical properties were engineered using an optimized freeze-dried extract and developed solid lipid nanoparticles (SLNs) as an effective drug-delivery system. An industrially viable and environment-friendly hot high-pressure homogenization technique led to a stable formulation with an average particle size of 178.4 nm, as well as a 7-fold increase in loading and a significant entrapment of 91 ± 1.25%. The pharmacodynamic studies of developed nanosystems in excision-wound models showed faster and complete healing of wounds with no scars.

Nose to Brain Delivery of Astaxanthin-Loaded Nanostructured Lipid Carriers in Rat Model of Alzheimer's Disease: Preparation, in vitro and in vivo Evaluation.

Astaxanthin (AST) is a second-generation antioxidant with anti-inflammatory and neuroprotective properties and could be a promising candidate for Alzheimer's disease (AD) therapy, but is shows poor oral bioavailability due to its high lipophilicity. This study aimed to prepare and evaluate AST-loaded nanostructured lipid carriers (NLCs), for enhanced nose-to-brain drug delivery to improve its therapeutic efficacy in rat model of AD. AST-NLCs were prepared using hot high-pressure homogenization technique, and processing parameters such as total lipid-to-drug ratio, solid lipid-to-liquid lipid ratio, and concentration of surfactant were optimized. The optimized AST-NLCs had a mean particle size of 142.8 ± 5.02 nm, polydispersity index of 0.247 ± 0.016, zeta potential of -32.2 ± 7.88 mV, entrapment efficiency of 94.1 ± 2.46%, drug loading of 23.5 ± 1.48%, and spherical morphology as revealed by transmission electron microscopy. Differential scanning calorimetry showed that AST was molecularly dispersed in the NLC matrix in an amorphous state, whereas Fourier transform infrared spectroscopy indicated that there is no interaction between AST and lipids. AST displayed a biphasic release pattern from NLCs; an initial burst release followed by sustained release for 24 h. AST-NLCs were stable at 4-8 ±2°C for six months. Intranasal treatment of AD-like rats with the optimized AST-NLCs significantly decreased oxidative stress, amyloidogenic pathway, neuroinflammation and apoptosis, and significantly improved the cholinergic neurotransmission compared to AST-solution. This was observed by the significant decline in the levels of malondialdehyde, nuclear factor-kappa B, amyloid beta (Aβ1‑42), caspase-3, acetylcholinesterase, and β-site amyloid precursor protein cleaving enzyme-1 expression, and significant increase in the contents of acetylcholine and glutathione after treatment with AST-NLCs. NLCs enhanced the intranasal delivery of AST and significantly improved its therapeutic properties.

Formulation and Characterization of Febuxostat Loaded Nanostructured Lipid Carriers (NLCs) - Gel for Topical Treatment of Gout.

The aim of the present study was to formulate and characterize Nano- Structured Lipid Carriers (NLCs) of Febuxostat (FB) incorporated in the gel for the treatment of Gout. FB is a Xanthine Oxidase (XO) inhibitor drug used for chronic Gout and hyperuricemia. FB is a BCS class II drug, therefore, water solubility is very poor, and due to its poor solubility and wettability, it leads to poor dissolution. The hot high-pressure homogenization technique was used in this study to improve the physicochemical property of FB. The carbopol 934 was used to prepare NLCs gel of FB. The NLCs of FB was prepared in different drug: polymer ratios w/w (2:1), (1:1), (1:2), (1:3) and (1:4) with solid lipid (Stearic Acid) and liquid lipid (Oleic acid). The preformulation study of FB included FTIR study melting point, standard calibration curves, and drug-polymer interaction study. The NLCs (1:3) showed high entrapment and drug content. The NLCs gel formulation was 87% released within 6 hours in a controlled manner. NLCs gel modifies the drug release, increases the bioavailability, and reduces side effects of FB. The prepared gel is the efficient formulation for the better treatment of chronic gout and hyperuricemia. The research findings have shown the undesirable side effects associated with the oral route that can be reduced by the use of NLCs formulation through the transdermal route in an effective manner.

Eudragit S-100 Surface Engineered Nanostructured Lipid Carriers for Colon Targeting of 5-Fluorouracil: Optimization and In Vitro and In Vivo Characterization

5-Fluorouracil (5-FU) is the most preferred chemotherapeutic agent in the management of colon cancer but is associated with poor therapeutic efficacy and lack of site specificity. Hence, it was aimed to employ Eudragit S100 surface engineered 5-FU nanostructured lipid carriers for the spatial and temporal release of the drug for the treatment of colon cancer. Hot high-pressure homogenization (HPH) technique was employed in the preparation of 5-FU-NLCs. The optimization of 5-FU-NLCs was performed using a Quality by Design (QbD) approach. A 32 factorial design was employed wherein the relationship between independent variables [amount of oleic acid (X1) and concentration of Tween®80 (X2)] and dependent variables [particle size (Y1) and % entrapment efficiency (Y2)] was studied. Optimized 5-FU-NLCs were surface treated to obtain Eudragit S100-coated 5-FU-NLCs (EU-5-FU-NLCs). The evaluation parameters for 5-FU-NLCs and EU-5-FU-NLCs included surface morphology, particle size, PDI, and zeta potential. In vitro release from EU-5-FU-NLCs revealed a selective and controlled 5-FU release in the colonic region for 24 h. In vitro cytotoxicity (MTT assay) was performed against Caco-2 cancer cells, wherein EU-5-FU-NLCs exhibited a 2-fold greater cytotoxic potential in comparison to a 5-FU solution (5-FU-DS). Oral administration of EU-5-FU-NLCs in Albino Wistar rats depicted a higher Cmax (2.54 folds) and AUC (11 folds) as well as prolonged Tmax (16 folds) and MRT (4.32 folds) compared to 5-FU-DS confirming higher bioavailability along with the spatial and temporal release in the colonic region. Thus, a multifaceted strategy involving abridgement of nanotechnology along with surface engineering is introduced for effective chemotherapy of colon cancer via oral administration of 5-FU with uncompromised safety and higher efficacy.Graphical abstract.

Nanostructured lipid base carrier for specific delivery of garlic oil through blood brain barrier against aggressiveness of glioma

Glioblastoma, GBM, is a primary malignant brain tumor and is one of the most difficult-to-treat cancers. The inability of drugs to cross the blood brain barrier (BBB) is the main obstacle for treating brain cancers. The development of drug delivery systems which improve the permeation across the BBB is the focus of this research, specifically the benefits and use of nanostructured lipid carriers (NLC). The anti-inflammatory and anti-tumor activity of garlic oil have been widely studied. However, direct treatment with garlic oil is restricted due to its low bioavailability and the application of drug for brain cancer to improve the efficiency of garlic oil, a NLC was developed as a carrier of garlic oil. The garlic NLC was formulated using the hot high-pressure homogenization technique. The physicochemical properties of the garlic NLC were analyzed using dynamic light scattering. Size of the garlic NLC was 136.8 ± 0.56 nm and the zeta potentials of each formulation were −36.27 ± 0.96 mV and PDI 0.163 ± 0.03. The effect of garlic NLC on the cell viability of the glioma cell was determined using a MTT assay. The garlic NLC had higher efficiency towards inhibiting cell viability of glioma cells compared to free garlic oil. In addition, the effects of the garlic NLC on cell migration and cell invasion were assessed using a Boyden chamber assay. The migration and invasion abilities of garlic NLC treated cells were significantly decreased compared to the control and free garlic oil. Moreover, in vitro BBB was used to test permeation of garlic oil across BBB. Interestingly, garlic NLC could cross the BBB while the free garlic oil could not. Taken together, garlic NLC might be applicable as an alternative therapeutic treatment strategy for brain cancer.

Formulation and evaluation of nano structured lipid carriers for intranasal delivery of Buspirone hydrochloride

The aim of this work was to formulate buspirone hydrochloride (BH) NLCs for intranasal administration to improve BH bioavailability. The BH loaded NLCs were prepared by hot high-pressure homogenization technique using Precirol ATO 5, olive oil and tween 80 as solid lipid, liquid lipid and surfactant, respectively. Carbopol 934P and HPMC K4M were used to convert NLCs dispersion into NLCs based in-situ nasal gelling solution to improve its mucoadhesive property for intranasal administration. A factorial design approach was used to study the effect of independent variable (amount of Precirol ATO 5 and olive oil) on the dependent variables (particle size and percentage entrapment efficiency (%EE). The optimized formulation was characterized for particle size, zeta potential, %EE, and surface morphology. Fourier transform infrared (FTIR) spectroscopy was used to study the possible BH-lipid complex formation. Further, viscosity determination, stability studies, in-vitro drug release, ex-vivo skin permeation studies and ex-vivo nasal toxicity studies of BH loaded NLCs nasal gelling solution were carried out. The BH loaded NLCs (batch F8) showed particle size of 111.8nm, %EE of 78.34% and zeta potential of-44.3mV. Scanning electron microscopy (SEM) confirmed spherical shape of NLCs. In vitro drug release and ex vivo skin permeation studies of BH loaded NLCs and BH loaded NLCs in-situ nasal gelling solution showed 71.26% drug permeation.

Loading, release profile and accelerated stability assessment of monoterpenes-loaded solid lipid nanoparticles (SLN)

Glycerol monostearate solid lipid nanoparticles (SLN) were produced by hot high-pressure homogenization technique to load alpha-pinene, citral, geraniol or limonene. SLN were composed of 1 wt.% monoterpene, 4 wt.% of Imwitor® 900K as a solid lipid and 2.5 wt.% of Poloxamer188 as a surfactant. Empty SLN consisted of 5 wt.% of Imwitor® 900K and 2.5 wt.% of Poloxamer188. The mean particles size (Z-Ave) and polydispersity index (PDI) of SLN were analyzed by dynamic light scattering (DLS), while the zeta potential (ZP) of each formulation were measured by electrophoretic light scattering. LUMiSizer® was applied to calculate the velocity distribution in the centrifugal field and instability index. Drug release profile from SLN was analyzed using Franz cell diffusion cells assayed by UV–Vis spectrophotometry, whereas the gas chromatography technique was applied to determine the encapsulation parameters of volatile monoterpenes. The matrix state, polymorphism and phase behavior of SLN were studied by X-ray diffraction (XRD, low and wide angles) and differential scanning calorimetry (DSC). Selected monoterpenes were successfully loaded in glycerol monostearate SLN. A burst release profile within the first 15 min was observed for all formulations, being the modified release profile dependent on the type of monoterpene and on the encapsulation efficiency.

Sucupira Oil-Loaded Nanostructured Lipid Carriers (NLC): Lipid Screening, Factorial Design, Release Profile, and Cytotoxicity.

Essential oils are odorant liquid oily products consisting of a complex mixture of volatile compounds obtained from a plant raw material. They have been increasingly proven to act as potential natural agents in the treatment of several human conditions, including diabetes mellitus (DM). DM is a metabolic disorder characterized by chronic hyperglycemia closely related to carbohydrate, protein and fat metabolism disturbances. In order to explore novel approaches for the management of DM our group proposes the encapsulation of sucupira essential oil, obtained from the fruits of the Brazilian plants of the genus Pterodon, in nanostructured lipid carriers (NLCs), a second generation of lipid nanoparticles which act as new controlled drug delivery system (DDS). Encapsulation was performed by hot high-pressure homogenization (HPH) technique and the samples were then analyzed by dynamic light scattering (DLS) for mean average size and polydispersity index (PI) and by electrophoretic light scattering (ELS) for zeta potential (ZP), immediately after production and after 24 h of storage at 4 °C. An optimal sucupira-loaded NLC was found to consist of 0.5% (m/V) sucupira oil, 4.5% (m/V) of Kollivax® GMS II and 1.425% (m/V) of TPGS (formulation no. 6) characterized by a mean particle size ranging from 148.1 ± 0.9815 nm (0 h) to 159.3 ± 9.539 nm (at 24 h), a PI from 0.274 ± 0.029 (0 h) to 0.305 ± 0.028 (24 h) and a ZP from −0.00236 ± 0.147 mV (at 0 h) to 0.125 ± 0.162 (at 24 h). The encapsulation efficiency and loading capacity were 99.98% and 9.6%, respectively. The optimized formulation followed a modified release profile fitting the first order kinetics, over a period of 8 h. In vitro cytotoxicity studies were performed against Caco-2 cell lines, for which the cell viability above 90% confirmed the non-cytotoxic profile of both blank and sucupira oil-loaded NLC.

Thermo-reversible in situ forming implant with nanostructured lipid carriers (NLC) as a delivery system for the administration of estradiol valerate.

A thermo-reversible in situ forming implant, based on the combination of Pluronic® F-127 and Pluronic® F-68 with nanostructured lipid carriers (NLC), was formulated with the aim of achieving the sustained release of estradiol valerate (EV). EV-loaded NLC, prepared by the hot high-pressure homogenization technique, presented an entrapment efficiency of 90 ± 2.9%, a particle size (PS) of 122 ± 11.2nm, a polydispersity index (PDI) of 0.344 ± 0.07, and a zeta potential (ZP) of - 10.5 ± 1.3mV. Once obtained, NLC were then included in a thermo-reversible gel (EV-loaded NLC gel), which was characterized by its rheological behavior, gelation temperature, and injectability. The in vitro release tests showed that the EV-loaded NLC gel delayed the release significantly, in comparison with a solution of the drug and with the EV-loaded NLC. The EV-loaded NLC gel and a commercially available suspension containing estradiol were administered parenterally to rabbits. A 16.8-fold greater AUC and a 40-fold higher Cmax were obtained with the EV-loaded NLC gel, compared to the commercial suspension. A rapid initial release of EV in vivo, from the EV-loaded NLC gel, suggests that it is necessary to adjust the ratio of the copolymers or to include in the gel an additive that improves gelation time and gel strength, in order to achieve a sustained release. An interesting observation was that the in vitro profile, which has a three-phase behavior, coincides with what was observed in the in vivo study. Graphical abstract.

Development and Optimization of Alpha-Pinene-Loaded Solid Lipid Nanoparticles (SLN) Using Experimental Factorial Design and Dispersion Analysis.

The encapsulation of bicyclic monoterpene α-pinene into solid lipid nanoparticles (SLN) is reported using experimental factorial design, followed by high-end dispersion analyzer LUMiSizer®. This equipment allows the characterization of the α-pinene-loaded SLN instability phenomena (e.g., sedimentation, flotation or coagulation), as well as the determination of the velocity distribution in the centrifugal field and the particle size distribution. In this work, SLN were produced by hot high-pressure homogenization technique. The influence of the independent variables, surfactant and lipid ratio on the physicochemical properties of SLN, such as mean particle size (Z-Ave), polydispersity index (PDI) and zeta potential (ZP), was estimated using a 22-factorial design. The Z-Ave and PDI were analyzed by dynamic light scattering, while ZP measurements were recorded by electrophoretic light scattering. Based on the obtained results, the optimal SLN dispersion was composed of 1 wt.% of α-pinene, 4 wt.% of solid lipid (Imwitor® 900 K) and 2.5 wt.% of surfactant (Poloxamer 188), depicting 136.7 nm of Z-Ave, 0.170 of PDI and 0 mV of ZP. Furthermore, LUMISizer® has been successfully used in the stability analysis of α-pinene-loaded SLN.

Design of colloidal drug carriers of celecoxib for use in treatment of breast cancer and leukemia

Inflammation develops initiation and pathological process of cancer. Nanoscale drug carriers are required to be investigated for delivery of actives at cellular level for treatment of various cancer types. Solid lipid nanoparticles (CLX-SLN), nanostructured lipid carriers (CLX-NLC) and a nanoemulsion (CLX-NE) of celecoxib (CLX), a selective cyclooxygenase-2 inhibitor, were formulated for use in remedy of breast cancer and acute promyelocytic leukemia. The hot high pressure homogenization technique was employed to product formulations. Scanning electron micrographs were utilized for morphological characterization of formulations. Laser diffraction (LD), photon correlation spectroscopy (PCS) and differential scanning calorimetry (DSC) were used for examination of their physical stability by storing them at various temperatures. Drug release profiles of formulations were obtained. Their activity on cancer cells was investigated in the cell culture experiments. Stable formulations having homogenous size distribution were obtained below 200 nm with high drug payloads between 93.76% and 96.66%. Nanoparticles were ascertained to contribute controlled drug release. CLX-SLN induced the highest decrease in numbers of human breast cancer and human acute promyelocytic leukemia cells through the activation of the cell death cascades especially apoptosis in comparison to CLX-NLC, CLX-NE and the pure CLX application (p < 0.05). Nanoformulations of CLX optimized in this study were found to have various advantages expected from sophisticated drug delivery systems in order to achieve higher CLX efficiency at cellular level. Thus, they are able to be administered efficaciously alone and in combination therapies in remedy of breast cancer and acute promyelocytic leukemia.

NLCs as a potential carrier system for transdermal delivery of forskolin.

Nanostructured lipid carriers (NLC) composed of the substances generally recognized as safe (GRAS) were obtained by using a hot high-pressure homogenization technique (HPH). The influence of the number of homogenization cycles and concentration of a decyl glucoside surfactant on the NLC properties were studied. The system's stability was assessed by macroscopic observation, light backscattering and zeta potential measurements. NLC particle size was measured using dynamic light scattering (DLS). The kinetically stable formulations were loaded with forskolin and selected for in vitro drug permeation study using the Franz cell method. Concentration of forskolin in the receptor solution (i.e. ethanol/PBS mixture) was analyzed with high performance liquid chromatography (HPLC) with UV detection. The obtained results have shown that NLC formulations could be used as effective carriers for forskolin permeation through the skin.

N,N,N‑trimethyl chitosan modified flaxseed oil based mucoadhesive neuronanoemulsions for direct nose to brain drug delivery

Here we fabricated flaxseed oil-based neuronanoemulsions (NNEs) which were further surface-modified with a mucoadhesive polymer, N,N,N‑trimethyl chitosan (TMC) to form mucoadhesive neuronanoemulsions (mNNEs). The NNEs were loaded with high partitioning ropinirole-dextran sulfate (ROPI-DS) nanoplex and fabricated using hot high-pressure homogenization (HPH) technique. NNEs were optimized using Central Composite experimental design. TMC modified mNNE have not been prepared yet for direct nose to brain drug delivery. Here, an objective to provide controlled drug release with prolonged residence on the nasal mucosa for the treatment of Parkinson's disease (PD) is at prime consideration. Enhanced brain targeting through BBB bypass drug delivery, improved therapeutic efficacy through enhanced retention of mNNE formulation over nasal mucosal membrane, reduced dose and frequency of administration, and safety were further expected outcomes of this experiment. The mNNE formulation was subjected to 6 month stability assessment. The mNNE formulation was administered to the Swiss albino mice model via intranasal route and both, the plasma and brain pharmacokinetics were estimated. The in vivo studies performed on mice exhibited high brain targeting efficiency of mNNE formulation through nose to brain delivery via olfactory pathway. The prepared intranasal mNNEs could be on the clinics, if investigated more for behavioral and neurotoxicity studies.

DEVELOPMENT AND CHARACTERIZATION OF PIPER RETROFRACTUM EXTRACT LOADED MUCOADHESIVE NANOSTRUCTURED LIPID CARRIERS FOR TOPICAL ORAL DRUG DELIVERY

Objective: To develop and characterize Piper retrofractum extract loaded nanostructured lipid carriers (PRE loaded NLCs) for topical oral cavity administration to enhance bioavailability and stability of piperine.Methods: PRE loaded NLCs were prepared with a hot high-pressure homogenization technique followed by coating the particle surface with mucoadhesive polymers; polyethene glycol 400 (PEG) and polyvinyl alcohol (PVA). The physicochemical properties in terms of particle size, polydispersity index, zeta potential, drug entrapment efficiency, in vitro drug release profile and antimicrobial activities were examined. In vitro, mucoadhesion studies were assessed by the wash-off test. The physicochemical stabilities of mouth spray containing PRE loaded NLCs were investigated by kept at room temperature and 4 °C for 6 mo.Results: The PRE loaded NLCs showed spherical shape with a mean particle size of ~100-120 nm and zeta potential of ~-24 mV. Up to 90% drug entrapment efficiency was achieved. PEG-NLCs and PVA-NLCs showed a strong interaction with porcine buccal mucosa than uncoated-NLCs. All PRE loaded NLCs formulations revealed fast release characteristics and effective against Streptococcus mutans and S. sanguinis. The mouth spray containing PRE loaded NLCs showed good physical stability without particle aggregation. In addition, the chemical stability of piperine in NLCs was significantly improved during storage at both storage conditions compared to its solution form.Conclusion: The developed PRE loaded polymer coated-NLCs showed high potential to use as a local drug delivery system for reducing the bacterial growth in the oral cavity.

Prolonged Release and Cytocompatibility on Immortalized Keratinocytes of CoQ10-Loaded Nanostructured Lipid Carrier

The objective was to manufacture a nanostructured lipid carrier (NLC) for Coenzyme Q10, and to investigate its prolonged release and cytocompatibility of CoQ10-NLC incubated with HaCaT cells. CoQ10-NLC was prepared by hot high-pressure homogenization technique. The characterization of the CoQ10-NLC was determined by size analysis, polydispersity index (PDI), zeta potential assay, in vitro release and cytocompatibility. To analyze the cytocompatibility of CoQ10-NLC, cell viability was investigated by MTT measurement. Morphology of cells was evaluated by HE staining. Cells were exposed to CoQ10-NLC and nuclear morphology were determined using Hoechst 33342 staining. Time-lapse imaging was used to illustrate the dynamics of cell movements. Release investigation exhibited a prolonged release of CoQ10-NLC. MTT measurement, HE and Hoechst 33342 staining corroborated that CoQ10-NLC possessed good cytocompatibility on HaCaT cells. Observation with time-lapse images further confirmed that CoQ10-NLC showed good cytocompatibility. The results demonstrated that CoQ10-NLC with prolonged release had good cytocompatibility.

Thymoquinone-loaded nanostructured lipid carrier exhibited cytotoxicity towards breast cancer cell lines (MDA-MB-231 and MCF-7) and cervical cancer cell lines (HeLa and SiHa).

Thymoquinone (TQ) has been shown to exhibit antitumor properties. Thymoquinone-loaded nanostructured lipid carrier (TQ-NLC) was developed to improve the bioavailability and cytotoxicity of TQ. This study was conducted to determine the cytotoxic effects of TQ-NLC on breast cancer (MDA-MB-231 and MCF-7) and cervical cancer cell lines (HeLa and SiHa). TQ-NLC was prepared by applying the hot high pressure homogenization technique. The mean particle size of TQ-NLC was 35.66 ± 0.1235 nm with a narrow polydispersity index (PDI) lower than 0.25. The zeta potential of TQ-NLC was greater than −30 mV. Polysorbate 80 helps to increase the stability of TQ-NLC. Differential scanning calorimetry showed that TQ-NLC has a melting point of 56.73°C, which is lower than that of the bulk material. The encapsulation efficiency of TQ in TQ-NLC was 97.63 ± 0.1798% as determined by HPLC analysis. TQ-NLC exhibited antiproliferative activity towards all the cell lines in a dose-dependent manner which was most cytotoxic towards MDA-MB-231 cells. Cell shrinkage was noted following treatment of MDA-MB-231 cells with TQ-NLC with an increase of apoptotic cell population (P < 0.05). TQ-NLC also induced cell cycle arrest. TQ-NLC was most cytotoxic towards MDA-MB-231 cells. It induced apoptosis and cell cycle arrest in the cells.

Influence of vegetable oil on the synthesis of bioactive nanocarriers with broad spectrum photoprotection

Abstract Due to their unique features, most nanostructured lipid carriers (NLCs) in association with vegetable oils that exhibit UV filtering properties and bioactivity could be used in many cosmetic formulations. Therefore, in this work, a new application of pomegranate seed oil (PSO) in the cosmetic sector was developed, based on the synthesis of bioactive lipid nanocarriers loaded with various UV filters by the hot high pressure homogenization technique. To get broad spectrum photoprotection, different UVA and UVB filters have been used (Avobenzone — AVO, Octocrylen-OCT, Bemotrizinol — BEMT). The influence of the solid lipids combined with PSO on the particle size, physical stability and entrapment efficiency was investigated using 8 nanocarrier systems. An improved physical stability and an appropriate size were obtained for NLCs prepared with Emulgade, carnauba wax and PSO (e.g. −30.9÷-36.9 mV and 160÷185 nm). NLCs showed an entrapment efficiency above 90% and assured slow release rates of UV filters, especially for BEMT (5%). The developed nanocarriers have been formulated into safe and effective sunscreens containing low amounts of synthetic UV filters coupled with a high percent of natural ingredients. The highest SPF of 34.3 was obtained for a cream comprising of 11% PSO and 3.7% BEMT

Alpha-lipoic acid-loaded nanostructured lipid carrier: sustained release and biocompatibility to HaCaT cells in vitro

ALA-loaded nanostructured lipid carrier (ALA-NLC) was designed to improve physicochemical stability and water solubility, and promote sustained release of ALA as well as determine the biocompatibility of ALA-NLC. The ALA-NLC manufactured using hot high-pressure homogenization technique was investigated in terms of size, zeta potential, FTIR analysis and release behavior. In vitro cytotoxicity and biocompatibility were determined by incubating with HaCaT cells using the MTT assay, HE staining and Hoechst 33342 staining. Cell behavior and cellular division of HaCaT cells untreated and treated by ALA-NLC were investigated in real-time images gathered using time-lapse imaging system. The release investigation illustrated that only 6.9% of ALA released in 30 min from ALA-NLC formation, whereas it was 30.3% in free ALA system. ALA-NLC possessed a satisfactory release behavior of sustained release up to 72 h. It showed that ALA-NLC did not exert hazardous effect on HaCaT cells up to 81.9 mg/L without morphological alterations, revealing a satisfactory biocompatibility. Evidence was provided from time-lapse imaging system that cell behavior and cellular division of ALA-NLC treated HaCaT cells were in accordance with the control. These results of this investigation demonstrated that NLC encapsulated ALA formation (ALA-NLC) can improve stability, solubility and release of ALA; ALA-NLC was biocompatible to HaCaT cells.

Enhanced photoprotection for photo-labile compounds using double-layer coated corn oil-nanoemulsions with chitosan and lignosulfonate

With the aim to establish a novel nanocarrier system with relatively high payload and high photoprotection capacity for photo-labile active compounds, in this work, deltamethrin (photo-labile compound) was encapsulated into corn oil-nanoemulsions (NE) by a hot high pressure homogenization technique followed by coating with chitosan as the first coating layer (CH-NE) and lignosulfonate as the second coating layer to form a double-layer coated NE (L-CH-NE). The optimal conditions for preparation of NE, chitosan coating and lignosulfonate coating were investigated. The results indicate that polymer coating and the number of coating layers significantly affected the release profile and photoprotection capacity of nanocarriers. In particular, after coating, the release rate became slower and photoprotection capacity became higher. Moreover, in the case of L-CH-NE after 24h of UV exposure in direct photolysis and 2.5h of UV exposure in indirect photolysis, the non-degraded amount of deltamethrin was approximately 4.5 times and 2.1 times, respectively, higher than that of the free-from deltamethrin. In the future, this novel nanocarrier system will show great potential and be widely applied to many fields related to protection of photo-labile compounds against photo-degradation.

Design and Evaluation of Miconazole Nitrate loaded Nanostructured Lipid Carriers (NLC) for improving the Antifungal therapy

The aim of this study was to prepare and evaluate gels incorporating nanostructured lipid carriers (NLC) of Miconazole nitrate (MN) for systemic delivery of the active after topical application. MN has been used as model drugs to be incorporated into nanostructured lipid carriers, once they are very well established as antimycotics for the treatment of topical fungal infections. NLC designed for topical administration of MN, were prepared by the hot high pressure homogenization technique. This MN-NLC was characterized for particle size, entrapment efficiency, and SEM. The lipid nanoparticles were incorporated in gels for convenient topical application and were evaluated forfor particle size, Rheological analysis Texture analysis , In vitro drug release studies and Ex Vitro skin permeation Studies. The preparation of aqueous NLC dispersions with a mean particle size lower than 300 nm has been obtained with uniform size distribution (PI < 0.350). The prepared semi-solid systems showed mean particle size remained lower than 250 nm and PI remained lower than 0.500 after 3 months of storage. An initial rapid release was observed in the case of Marketed gel, whereas MN- NLC Gel depicted a slow initial release with a lag time of 0.5 h and 1 h, respectively. High amount of MN release was facilitated through abdominal skin of rats from marketed gel than MN-NLC Gel. Research work could be concluded as successful development of MN-loaded NLC-bearing hydrogel to increase the encapsulation efficiency of colloidal lipid carriers with advantage of improved performance in terms of stability and provides a sustaining MN topical effect as well as faster relief from fungal infection.