Solid Lipid Nanoparticles Dispersions Research Articles

“Characterization and stability of α-tocopherol loaded solid lipid nanoparticles formulated with different fully hydrogenated vegetable oils”

Solid lipid nanoparticles can be compatible with several bioactive compounds and confer a differentiated crystalline structure. This study aimed to produce α-tocopherol loaded solid lipid nanoparticles with fully hydrogenated oils and fats from palm oil, soybean oil, and crambe oil, by high-pressure homogenization, using lecithin as an emulsifier. After recrystallization of solid lipid nanoparticles, dispersions were evaluated until 60 days of storage for particle size, polydispersity index, zeta potential, microstructure, dispersion stability and α-tocopherol quantification. α-tocopherol loaded solid lipid nanoparticles showed particle sizes and zeta potential values considered adequate for this type of particle. Presence of α-tocopherol altered thermal behavior of the particles, leading to increased crystallinity, with no changes in polymorphism, when compared to the unloaded solid lipid nanoparticles. All α-tocopherol loaded solid lipid nanoparticles dispersions showed stability with no losses of α-tocopherol, indicating their potential as a carrier for this compound in fortified foods.

Quercetin Loaded Cationic Solid Lipid Nanoparticles in a Mucoadhesive In Situ Gel-A Novel Intravesical Therapy Tackling Bladder Cancer.

The study aim was to develop an intravesical delivery system of quercetin for bladder cancer management in order to improve drug efficacy, attain a controlled release profile and extend the residence time inside the bladder. Either uncoated or chitosan coated quercetin-loaded solid lipid nanoparticles (SLNs) were prepared and evaluated in terms of colloidal, morphological and thermal characteristics. Drug encapsulation efficiency and its release behaviour were assessed. Furthermore, cytotoxicity of SLNs on T-24 cells was evaluated. Ex vivo studies were carried out using bovine bladder mucosa. Spherical SLNs (≈250 nm) ensured good entrapment efficiencies (EE > 97%) and sustained drug release up to 142 h. Cytotoxicity profile revealed concentration-dependent toxicity recording an IC50 in the range of 1.6-8.9 μg/mL quercetin. SLNs were further dispersed in in situ hydrogels comprising poloxamer 407 (20%) with mucoadhesive polymers. In situ gels exhibited acceptable gelation temperatures (around 25 °C) and long erosion time (24-27 h). SLNs loaded gels displayed remarkably enhanced retention on bladder tissues relative to SLNs dispersions. Coated SLNs exhibited better penetration abilities compared to uncoated ones, while coated SLNs dispersed in gel (G10C-St-QCT-SLNs-2) showed the highest penetration up to 350 μm. Hence, G10C-St-QCT-SLNs-2 could be considered as a platform for intravesical quercetin delivery.

BIOAVAILABILITY ENHANCEMENT OF REPAGLINIDE USING NANO LIPID CARRIER: PREPARATION CHARACTERIZATION AND IN VIVO EVALUATION

Objective: The aim of this study to manufacture the prolonged release lipid nanoparticle (Solid lipid nanoparticle and nanostructure lipid carrier) of repaglinide for enhance the oral bioavailability. Methods: Solid lipid nanoparticles (SLN) and Nanostructured lipid carriers (NLC) were prepared by slight modification in the solvent diffusion method. The core material used as cetyl alcohol while blend with oleic acid was used in the preparation of NLC dispersion. Tween 80 were utilized as a Surfactant and lecithin as a cosurfactant in both types of lipid formulation. Lipid nanoparticles were characterized for size distribution, entrapment parameter, zeta potential, surface morphology, in vitro drug release and stability study. Pharmacodynamic study were also performed to evaluate the antidiabetic activity of repaglinide-loaded lipid nanodispersion. Results: It was observed that lipid matrix-based SLN and NLC having significant particle size (157.8±15.8 nm for NLC and 238.4±48.2 nm for SLN dispersion), entrapment efficacy 79.82±0.84% for NLC and 72.04±1.03% for SLN dispersion. Zeta potential report was also clarifying that the formulation is in a stable state for a prolong time. SEM study size distribution of particle as evaluated by Malvern instrument. The formulation was also confirmed to be stable after 180 d of storage, according to the data from the stability study. The in vivo antidiabetic assessment showed that Repaglinide-loaded SLN and NLC dispersion were able to reduce the blood sugar level. Interestingly, in the case of the RPG-SLN, RPG-NLC-I and RPG-NLC-II groups, and the average blood sugar values at all-time intervals were significantly less than that of the basal glucose value (p<0.05). Conclusion: The prepared SLN and NLC dispersion having the ability to control the release and make nano formulation suitable to resolve poor bioavailability of repaglinide.

Overview on Solid Lipid Nanoparticle for Topical Delivery and its Inevitable Applications

Solid lipid nanoparticle is a novel approach for topical drug delivery. As lipids used in preparation of solid lipid nanoparticles (SLN) will also get absorbed in skin layers, enhancing permeation across the biological membranes. For the stability of SLN dispersion, several surfactants were used. Mechanism incorporating for the preparation of SLN also impacts particle size and stability. Since the mechanism of SLN through the biological membrane is still under research as it may follow various skin penetration pathways. This review suggests the various method of preparation, common pathways of skin permeation, lipids and surfactant utilized in the production of SLN.

Твердые липидные наночастицы со стеариновой кислотой, стабилизированные стеаратом иттрия

In this work, we studied the effect of yttrium stearate on the physicochemical properties of dispersions of solid lipid nanoparticles composed of stearic acid stabilized with nonionic surfactants (Tween 60, Span 60). The results showed that an increase in the concentration of yttrium stearate leads to increasing kinetic stability and decreasing the average size of the aggregates. Along with this, the average size of single particles remains practically unchanged and amounts to 35±5 nm.

Development of Mupirocin- Tinidazole solid- Lipid Nanoparticles Loaded Topical gel for the Management of Bacterial Wound Infections

Solid lipid nanoparticles (SLNs) are novel drug carrier system which consists of a solid matrix composed of a lipid being solid at both room and body temperatures with a mean Particle Size (PS) between 50 and 1000 nm Mupirocin -Tinidazole solid-lipid nanoparticles were prepared using hot homogenization technique using Glyceryl monosterate, Stearic acid, Tween 80 and Poloxamer 188 using hot homogenization technique. Size of the nanoparticles was in the range of 83 to 211 nm with the zeta potential values between -2.1 to -5.2. Atomic Force Microscopy (AFM) confirms the spherical shape of solid lipid nanoparticles. Entrapment efficiency was best in the F1 formulation. In vitro release of the pure drug was found to be 75% of mupirocin and 66.5% of tinidazole at the end of 1 hr. Drug release from SLNs dispersion followed Korsermeyrs peppas-model, indicating fickian diffusion drug release, while that from the gel followed non Fickian model drug release. Antibacterial activity of the SLNs was less but the SLNs based gel shows no significant difference in activity to that of standard drug gentamycin against aerobic bacteria. The SLNs dispersion exhibited physicochemical stability under refrigeration upto 45 days without significant difference in particle size. Best formulation was developed into a topical gel using sodium alginate and it was evaluated for pH, viscosity, spreadbility, extrudability, bloom strength, Minimum Inhibitory Concentration (MIC) and Methicillin resistant staphylococcus aureus (MRSA). Extrudability and spreadability parameters of the gel are similar to that of marketed Mupirocin 2% cream formulation

Solid lipid nanoparticles: Influence of composition, fabrication methods and problems, in vitro drug release and intranasal administration provide to access olfactory bulb pathway for SLNs

Background: Solid lipid nanoparticles (SLN) have drawn increasing interest in recent years. These nanoparticles are formed from stable or solid lipid mixtures and then stabilized by emulsifiers. As nanoparticles, colloidal particles running in size somewhere in the 10 to 1000 nm range are known. SLN provides fascinating properties, such as minimal scale, massive surface area, high medication piling, correspondence of stages at the interface, and is interested in their ability to enhance drug execution. Main text: This paper provides a description of the choice of ingredients, the effect of lipids and their structure on the formulation, and the various methods of processing SLN. We explain the characteristics of SLN stability and the possibilities of SLN stabilization by lyophilization in this article. The relation between drug absorption and the complexity of SLN dispersions, which involves the existence of other colloidal structures and the physical state of the lipid, is uncommonly considered. We define the possible problems of SLN preparation and performance on the basis of characterization. First, the nasal route was known to accomplish the avoidance of first-pass hepatic metabolism in order to maximize absolute bioavailability, and secondly, the immediate nose-to-brain pathway to enhance the delivery of brain medicines. SLNs have been designated to increase drug permeability through the blood-brain barrier as a drug delivery device (BBB). Conclusion: To sum up, this article gives insight SLNs a colloidal drug carrier places together the compensations of polymeric nanoparticles, SLNs have numerous benefits such as easy incorporation of lipid and lipophilic as well as hydrophilic drugs, suitable physical stability, and available at low cost and easy to manufacture. The nasal route was accepted to exploit first its prevention of the hepatic first-pass metabolism to increase the absolute bioavailability, and second, the direct nose-to-brain pathway to enhance the brain drug delivery. SLNs were chosen as a drug delivery system to improve drug permeability across the blood-brain barrier (BBB) and consequently its brain delivery.

Enhancing Bioavailability and Stability of Curcumin Using Solid Lipid Nanoparticles (CLEN): A Covenant for Its Effectiveness.

Curcumin, very rightly referred to as “a wonder drug” is proven to be efficacious in a variety of inflammatory disorders including cancers. Antiaging, anti-inflammatory, antioxidant, antitumor, chemosensitizing, P-gp efflux inhibiting, and antiproliferative activity are some of the striking features of curcumin, highlighting its importance in chemotherapy. Curcumin inhibits Bcl-2, Bcl-XL, VEGF, c-Myc, ICAM-1, EGFR, STAT3 phosphorylation, and cyclin D1 genes involved in the various stages of breast, prostate, and gastric cancer proliferation, angiogenesis, invasion, and metastasis. The full therapeutic potential of curcumin however remains under explored mainly due to poor absorption, rapid metabolism and systemic elimination culminating in its poor bioavailability. Furthermore, curcumin is insoluble, unstable at various pH and is also prone to undergo photodegradation. Nanotechnology can help improve the therapeutic potential of drug molecules with compromised biopharmaceutical profiles. Solid lipid nanoparticles (SLNs) are the latest offshoot of nanomedicine with proven advantages of high drug payload, longer shelf life, biocompatibility and biodegradability, and industrial amenability of the production process. We successfully developed CLEN (Curcumin encapsulated lipidic nanoconstructs) containing 15 mg curcumin per ml of the SLN dispersion with highest (till date, to our knowledge) increase in solubility of curcumin in an aqueous system by 1.4 × 106 times as compared to its intrinsic solubility of 11 ng/ml and high drug loading (15% w/v with respect to lipid matrix). Zero-order release kinetics observed for CLEN versus first order release for free curcumin establish controlled release nature of the developed CLEN. It showed 69.78 times higher oral bioavailability with respect to free curcumin; 9.00 times higher than a bioavailable marketed formulation (CurcuWIN®). The formulation showed 104, 13.3, and 10-times enhanced stability at pH 6.8, 1.2, and 7.4, respectively. All these factors ensure the efficacy of CLEN in treating cancer and other inflammatory diseases.

Development of Mupirocin-Tinidazole solid-Lipid Nanoparticles Loaded Topical Gel for the Management of Bacterial Wound Infections

Solid lipid nanoparticles (SLNs) are novel drug carrier system which consists of a solid matrix composed of a lipid being solid at both room and body temperatures with a mean Particle Size (PS) between 50 and 1000 nm Mupirocin-Tinidazole solid-lipid nanoparticles were prepared using hot homogenization technique using Glyceryl monosterate, Stearic acid, Tween 80 and Poloxamer 188 using hot homogenization technique. Size of the nanoparticles was in the range of 83 to 211 nm with the zeta potential values between-2.1 to-5.2. Atomic Force Microscopy (AFM) confirms the spherical shape of solid lipid nanoparticles. Entrapment efficiency was best in the F1 formulation. In vitro release of the pure drug was found to be 75% of mupirocin and 66.5% of tinidazole at the end of 1 hr. Drug release from SLNs dispersion followed korsermeyrs peppas-model, indicating fickian diffusion drug release, while that from the gel followed non fickian model drug release. Antibacterial activity of the SLNs was less but the SLNs based gel shows no significant difference in activity to that of standard drug gentamycin against aerobic bacteria. The SLNs dispersion exhibited physicochemical stability under refrigeration up to 45 days without significant difference in particle size. Best formulation was developed into a topical gel using sodium alginate and it was evaluated for pH, viscosity, spreadbility, extrudability, bloom strength, Minimum Inhibitory Concentration (MIC) and Methicillin resistant staphylococcus aureus(MRSA). Extrudability and spreadability parameters of the gel are similar to that of marketed Mupirocin 2% cream formulation

Solid Lipid Nanoparticles of Dronedarone Hydrochloride for Oral Delivery: Optimization, In Vivo Pharmacokinetics and Uptake Studies.

Dronedarone HCl (DRD), owing to its poor aqueous solubility and extensive presystemic metabolism shows low oral bioavailability of about 4% without food, which increases to approximately 15% when administered with a high fat meal. Solid lipid nanoparticles (SLN) were designed with glyceryl monstearate (GMS) in order to improve oral bioavailability of DRD. Hot homogenization followed by probe sonication was used to prepare SLN dispersions. Box-Behnken design was used to optimize manufacturing conditions. SLN were characterized for particle size, zeta potential, entrapment efficiency, physical state and in vitro drug release. Pharmacokinetics and intestinal uptake study of dronedarone HCl loaded solid lipid nanoparticles (DRD-SLN) in the presence and absence of endocytic uptake inhibitor, chlorpromazine (CPZ) was performed with conscious male Wistar rats. Optimized formulation of SLN showed particle size of 233 ± 42 nm and entrapment efficiency of 87.4 ± 1.29%. Results of pharmacokinetic studies revealed enhancement of bioavailability of DRD by 2.68 folds from SLN as compared to DRD suspension. Significantly reduced bioavailability of DRD-SLNs in the presence of chlorpromazine, demonstrated the role of endocytosis in uptake of SLN formulation. These results indicated that dronedarone HCl loaded SLN could potentially be exploited as a delivery system for improving oral bioavailability by minimizing first pass metabolism.

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.

FORMULATION AND EVALUATION OF DASATINIB LOADED SOLID LIPID NANOPARTICLES

Objective: The aim of present work was to formulate and evaluate Dasatinib (DST) loaded solid lipid nanoparticles (SLNs) as a potential anticancer drug delivery system by enhancing its solubility.Methods: SLNs consist of a solid lipid matrix where the drug was incorporated. Surfactants of GRAS grade were used to avoid aggregation and to stabilize the SLNs. DST-SLNs formulations of varying concentrations were prepared by high speed homogenization technique and evaluated for drug excipients compatibility study, poly-dispersity index, particle size analysis, surface morphology, zeta potential and drug release features.Results: It was observed that DST-SLNs with optimum quantities of poloxomer: lecithin ratio showed 88.06% drug release in 6h with good entrapment efficiency of 76.9±0.84 %. Particle size, Poly dispersity index, zeta potential and drug entrapment efficiency for the optimized formulation was found to be optimum. Stability studies revealed that the entrapment efficiency of the SLN dispersion stored in 4 °C was stable.Conclusion: Thus, it can be concluded that formulations of DST loaded SLNs are suitable carriers for improving the solubility and dissolution related problems.

Development and In Vitro Characterization of Solid Lipid Nanoparticles(SLN) Containing Methotrexate And Doxycycline

Solid lipid nanoparticles (SLN) containing Disease Modifying Antirheumatic drugs (DMARDs) Methotrexate (MTX) and Doxycycline (DOX) was developed using a triglyceride (tristearin) and a polaxamer (pluronic F68). Hot homogenization of melted lipid and aqueous phase at temperature above the melting point of lipid had produced SLN dispersion. Optimization of process and formulation variables have yielded SLN having an entrapment efficiency of 65.07%±1.23% and 79.56%±0.92% for MTX and DOX respectively. Particle size and zeta potential measured using Malvern Zetasizer showed 157.2nm and -9.6mv respectively for the optimized SLN formulation. The compatibility between the drug and the formulation excipients was tested by Fourier Transform Infrared Spectroscopy (FTIR) and found to be compatible. Powder X-ray diffraction (PXRD) study revealed that the drugs and lipid were dispersed in crystalline state in SLN. The in vitro drug release studies performed in phosphate buffer of pH 7.4 using dialysis bag showed a sustained release of both the drugs (andgt;75%±1.4%) up to a period of two days. From the in vitro results, it can be concluded that SLN was found to be a suitable nano carrier for the incorporation of DMARDS: MTX and DOX without any significant interaction. The developed system produced sustained release of both the drugs (based on their concentration) for longer duration and thus suitable for the chronic inflammatory conditions of RA.

Optimization of linalool-loaded solid lipid nanoparticles using experimental factorial design and long-term stability studies with a new centrifugal sedimentation method

Linalool (C10H18O), also known as 3, 7-dimethyl-1, 6-octadien-3-ol, is the most common acyclic monoterpene tertiary alcohol present in essential oils of several aromatic plant species. Previous studies indicate that linalool is a valuable compound with a wide range of therapeutic properties. The promising therapeutic effects of linalool are however limited by its poor water solubility and volatility. Recently, the encapsulation of linalool in drug delivery systems, such as solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) has demonstrated to overcome linalool physicochemical limitations. The present study aimed the production and optimization of linalool encapsulation in SLN applying the experimental full factorial design. The estimation of the long-term stability of the produced linalool-loaded SLN was carried out using a new centrifugal sedimentation method, LUMiSizer®. SLN dispersions were produced by the hot high pressure homogenization (HPH) method. The influence of the independent variables, surfactant and lipid concentrations on linalool-loaded SLN particle size, polydispersity index (PI) and zeta potential (ZP) was evaluated by a 22 factorial design composed of 2 variables which were set at 2-levels each. For each of the three dependent variables, analysis of the variance (ANOVA) was performed using a 95% confidence interval. The concentration of surfactant, as well as, the interaction between the different concentrations of lipid and surfactant, hada statistically significant effect on the particle size and PI. Experimental factorial design has been successfully employed to develop an optimal SLN dispersion, requiring a minimum of performed experiments. Based on the obtained results, the optimal linalool-loaded SLN dispersion was composed of 1% (w/v) linalool 2% (w/v) of solid lipid and 5% (w/v) of surfactant. Furthermore, the stability analysis revealed that the produced linalool-loaded SLN dispersions have limited storage stability which can be easily overcome through the assembly of a polymeric coating on the SLN surface. LUMiSizer® has been successfully used in the kinetic analysis of linalool-SLN during accelerated storage time.

Acyclovir Solid Lipid Nanoparticles for Skin Drug Delivery: Fabrication, Characterization and In vitro Study.

The fractionated coconut oil based Solid Lipid Nanoparticles (SLNs) of Acyclovir (ACV) were fabricated in two batches by using Glyceryl mono stearate (GMS) and Lipoid S75 (Fat free soybean phospholipids with 70% phosphatidylcholine-Lipoid GmbH, Germany). The research was focused on developing ACV-SLN by using high pressure hot-homogenization technique. The ingredients were used in different concentrations and ratios to identify the best formulation design. The GMS with Fractionated coconut oil and Lipoid S75 with Fractionated coconut oil were used in various concentrations in formulation design to assess the impact on the fabrication and evaluation of SLNs. The SLNs were subjected to various characterization techniques such as XRD (X-Ray Diffraction), FTIR (Fourier transform infrared study), master sizer analysis and zeta potential. The mean particle size was determined by master sizer and zeta sizer. Transmission Electron Microscopy (TEM) was used as a tool to analyze the morphology and other features. The zeta potential and drug Entrapment Efficiency (EE%) were also determined. The drug release time profile was studied in vitro study with the utilization of dialysis membrane technique as well as by wistar rat skin. The most recent patents related to the current research topic were also discussed. The Zeta potential of the best formulation from GMS batch GNE5 was found to be -2.62mV as the preparation was very viscous with low zeta potential. The better results of Lipoid S75 batch LS4 were found to be 23.23mV which was within the recommended range. The formulations prepared with Lipoid S75, LS4 showed narrow distribution size of 53.46nm and the uniformity was found to be 14.1. The formulation LS4 demonstrated the lowest distribution with of 6.8, 14.5, 139.1nm respectively amongst all the formulations. SLN dispersions exhibited the average size in nano range. SLNs with small particle size found to have predetermined encapsulation efficiency and relatively high loading capacity and predetermined in vitro drugrelease profile. The lipoid S and Pluronic F68 nanoparticles are found to be superior to Conventional GMSand tween 80 nanoparticles in terms of particles size, stability and zetapotential.

Fluconazole-loaded solid lipid nanoparticles topical gel for treatment of pityriasis versicolor: formulation and clinical study

Solid lipid nanoparticles (SLNs) are very potential formulations for topical delivery of antifungal drugs. Hence, the purpose of this research was to formulate the well-known antifungal agent Fluconazole (FLZ)-loaded SLNs topical gel to improve its efficiency for treatment of Pityriasis Versicolor (PV). FLZ-SLNs were prepared by modified high shear homogenization and ultrasonication method using different concentration of solid lipid (Compritol 888 ATO, Precirol ATO5) and surfactant (Cremophor RH40, Poloxamer 407). The physicochemical properties and the in vitro release study for all FLZ-SLNs were investigated. Furthermore, the optimized FLZ-SLN formula was incorporated into gel using Carpobol 934. A randomized controlled clinical trial (RCT) of potential batches was carried out on 30 well diagnosed PV patients comparing to market product Candistan® 1% cream. Follow up was done for 4 weeks by clinical and KOH examinations. The results showed that FlZ-SLNs were almost spherical shape having colloidal sizes with no aggregation. The drug entrapment efficiency ranged from 55.49% to 83.04%. The zeta potential values lie between −21 and −33 mV presenting good stability. FLZ showed prolonged in vitro release from SLNs dispersion and its Carbapol gel following Higuchi order equation. Clinical studies registered significant improvement (p < .05) in therapeutic response (1.4-fold; healing%, 4-fold; complete eradication) in terms of clinical cure and mycological cure rate from PV against marketed cream. Findings of the study suggest that the developed FLZ loaded SLNs topical gels have superior significant fast therapeutic index in treatment of PV over commercially available Candistan® cream.

FORMULATION, DEVELOPMENT AND CHARACTERIZATION OF SOLID LIPID NANOPARTICLES OF GEMCITABINE HYDROCHLORIDE

Gemcitabine Hydrochloride is a BCS class III drug of choice in the treatment of cancer, as a single or in combination chemotherapy. However, its bioavailability is a major concern due to its short half-life. Solid lipid nanoparticles (SLN) of Gemcitabine Hydrochloride were prepared to enhance its bioavailability, hence anticancer activity. The Quality by Design approach was applied for the formulation of SLN. The Randomized 32 factorial design was used with responses of particle size and % entrapment efficiency (% EE). The optimized batch of Gemcitabine Hydrochloride loaded SLN containing 1gm of GMS as solid lipid, 1gm of Tween80: Sodium Taurocholate as surfactant:co-surfactant and 5mg of Gemcitabine Hydrochloride was prepared by high shear homogenization method followed by Probe sonication for 15min to form nanoparticulate SLN dispersion. The Optimized batch of Gemcitabine Hydrochloride loaded SLN that exhausted mean particle size of 126.1nm, zeta potential -28.6 mV and % EE 74.83% respectively. SEM studies revealed three-dimensional nature of SLN with a slightly rough surface. DSC, results exhibited entrapment of Gemcitabine Hydrochloride in SLN. The optimized batch of SLN was evaluated for in-vitro % drug release using cellulose membrane dialysis bags for 24hrs and showed 63.13% CDR at 24 hrs. Anticancer cell line studies were also performed in human lung cancer cell line (A-549). It concludes that Gemcitabine Hydrochloride loaded Solid lipid Nanoparticles was successfully formulated and evaluated to sustain the drug release by bypassing the first pass metabolism. Key words: Gemcitabine Hydrochloride, SLN, QbD, High shear homogenization, anticancer activity.Â

Impact of Pluronic F-68 vs Tween 80 on Fabrication and Evaluation of Acyclovir SLNs for Skin Delivery

The solid lipid nanoparticles (SLNs) of Acyclovir (ACV) were fabricated with Soya lecithin and Fractionated Coconut oil (medium chain glyceride) as a first time combination. The research was focused on developing ACV-SLN by using high pressure hot-homogenization technique. The ingredients were used in different concentrations and ratios to identify the best formulation design. The tween 80 and Pluronic F-68 were used in various concentrations in formulation design to assess the impact on the fabrication and evaluation of SLNs. The impact of nanotechnology gain to play a vital role in the topical pharmaceutical products and the related patents will play a significant role in related industries. The SLNs were subjected to various characterization techniques such as XRD, FTIR, Master sizer analysis and zeta potential. The mean particle size was determined by master sizer and zeta sizer. Transmission electron microscopy (TEM) was used as a tool to analyze the morphology and other features. The zeta potential and drug entrapment efficiency (EE%) were also determined for the prepared ACV-SLNs. The efficiency of drug release from prepared formulations was studied by using in vitro study with the utilization of dialysis membrane technique. SLN dispersions exhibited the average size in nano range. SLNs with small particle size found to have predetermined encapsulation efficiency, and relatively high loading capacity and predetermined in vitro drug release profile.

Superoxide Dismutase-Loaded Solid Lipid Nanoparticles Prepared by Cold Homogenization Method: Characterization and Permeation Study Through Burned Rat Skin

Background: Superoxide dismutase (SOD), which inhibits lipid peroxidation and scavengers oxygen radicals, is an effective enzyme for treatment of skin ulcer lesion especially due to burns. Superoxide Dismutase is a hydrophilic compound with high molecular weight and low affinity for partitioning into skin. Moreover, another important limitation for its use in medicine is thermal denaturation and inactivation. Objectives: We developed solid lipid nanoparticles (SLN) dispersions for enhancing superoxide dismutase penetration across burned rat skin and enzyme protection against environmental degradation. Methods: Solid lipid nanoparticles were prepared with cold homogenization method because SOD is a thermo sensitive compound. The characteristics of SLNs such as particle size, entrapment efficiency and enzyme release pattern and permeability through burned rat skin were evaluated. Results: Solid lipid nanoparticles showed more than 90% entrapment efficiency and particle size lower than 102 nm. In vitro release study demonstrated SOD burst and sustained release characters in this manner with maximum of 65% of enzyme released after 48 hours. The SOD activity was measured and results indicated that SLN could protect activity of the enzyme. Differential scanning calorimetry of SLNs showed low crystalinity index percentage that is a reason for high entrapment efficiency and burst release character. Conclusions: The results indicated that SOD-loaded in SLN was delivered into deep burned skin layer and induced high enzyme activity through the skin. Low particle size, application of lecithin as surfactant and low crystallinity index (CI) percentage were important factors for increasing SOD penetration through the burned rat skin. Percentage of activity by SLN dispersions through rat skin was 13 folds more than the control.

Synergic Antibacterial Effect of Curcumin with Ampicillin; Free Drug Solutions in Comparison with SLN Dispersions.

Purpose: This study was designed to investigate benefit of using nanotechnology on increasing of synergic antibacterial effect of natural and chemical antibacterial agents. Methods: At first the MIC and MBC of Curcumin and Ampicillin as selected antibacterial agents was determined, after that Solid Lipid Nanoparticles (SLNs) of each active ingredients as well as Curcumin-Ampicillin loaded SLNs were prepared using high pressure homogenization technique. Characterization of prepared SLNs was done, then MIC, MBC and contact killing time were investigated for Curcumin-Ampicillin loaded SLNs in comparison with free Curcumin and Ampicillin solutions as well as Ampicillin and Curcumin SLNs. Results: Based on results nanoparticles with the size of 150 nm show much more decreased MIC and MBC when Ampicillin and Curcumin were loaded together on SLNs than solutions in which free Ampicillin and Curcumin were mixed. Conclusion: It seems that using nanotechnology could cause decrease the dosage of antibiotics and risk of having antibiotic resistance bacteria strains.