Metal ion-assisted drug-loading model for novel delivery system of cisplatin solid lipid nanoparticles with improving loading efficiency and sustained release

Objective: This study was aimed to design and characterize Paclitaxel-loaded Solid Lipid Nanoparticles (SLNs) to achieve site specificity,reduce toxicity and sustained release pattern. Methods: Paclitaxel-loaded solid lipid nanoparticles were fabricated by microemulsion followed by probe sonication technique using stearic acid as lipid and stabilized of the mixture of surfactants. In this study, 32 full factorial design was employed for optimizing the concentration of lipid as stearic acid and surfactant (soya lecithin) for the nanoparticles. The optimization was done by studying the dependent variable of particle size and % entrapment efficiency. Results: The results showed that the paclitaxel-loaded solid lipid nanoparticles prepared with the concentration of 33.31 % stearic acid and 500 mg of soya lecithin were optimum characteristic than other formulations. They showed the average particles size 149±4.10 nm and PDI 250±2.04. The zeta potential, % EE and % drug loading capacity was found to be respectively-29.7, 93.38±1.90 and 0.81±0.01. The optimized batch of Paclitaxel SLNs exhibited spherical shape with smooth surface analyzed by Transmission Electron Microscopy. In vitro study showed sustained release profile and was found to follow Higuchi Kinetics Equation. Conclusion: The SLNs of paclitaxel m et al. l the requirements of a colloidal drug delivery system. They had a particle size in nanosize; their size distribution was narrow and all the particles were in a spherical shape.

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NANOSTRUCTURED LIPID CARRIERS: A PROMISING APPROACH FOR TOPICAL DRUG DELIVERY SYSTEM

International Journal of Pharmaceutical Sciences and Medicine ◽

10.47760/ijpsm.2021.v06i07.007 ◽

2021 ◽

Vol 6 (7) ◽

pp. 81-101

Author(s):

Nikam Supriya S. ◽

Phadatare Priya P. ◽

Watode Ankita B. ◽

Kalyani Kayande

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Solid Lipid Nanoparticles ◽

Drug Loading ◽

Lipid Nanoparticles ◽

Local Effect ◽

Nanostructured Lipid Carriers ◽

Skin Hydration ◽

Solid Lipid

Nanostructured lipid carriers (NLCs) are innovative pharmaceutical formulations made up of physiological and biocompatible lipids, as well as surfactants and co-surfactant. The initial generation of lipid nanoparticles was Solid Lipid Nanoparticles (SLN), which had a longer-lasting activity and was better, suited to drug penetration. The NLC is a second-generation lipid nanoparticle designed to alleviate the limitations of SLN, such as limited drug loading capacity and solid lipid polymorphism. Many benefits of topical medication delivery include avoiding first-pass metabolism, focusing active components for a local effect, and patient compliance. When compared to typical topical dose forms, nanoparticles have a greater effect in transporting medications through the skin. The structure, composition, many formulation methods, and characterization of NLCs are all important aspects in formulating a stable drug delivery system, as discussed in this review paper. A variety of approaches are used to make solid lipid nanoparticles and nanostructured lipid carriers, which are discussed in this paper. Lipid nanoparticles have a variety of features that make them suitable for topical usage in cosmetics and medicinal formulations. Because of extensive positive benefits such as skin hydration, skin occlusion, and skin targeting, NLCs have a significant potential in the pharmaceutical market. Skin hydration is important for API topical distribution because it hydrates the skin, which causes the pores to open. Trans epidermal water loss decreases due to the occlusion nature of lipid nanoparticles, softening the skin. It is more suited since it uses biodegradable grade lipid, which does not cause toxicity like polymeric Nano formulations. Actually, because of their biodegradable composition, NLCs are a “Nano safe” carrier that has a lot of potential for overcoming the obstacles of topical distribution.

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Diazepam Loaded Solid Lipid Nanoparticles: In Vitro and in Vivo Evaluations

Advanced Pharmaceutical Bulletin ◽

10.34172/apb.2022.008 ◽

2020 ◽

Author(s):

Sara Faghihi ◽

Mohammad Reza Awadi ◽

Seyyedeh Elaheh Mousavi ◽

Seyyed Mahdi Rezayat Sorkhabadi ◽

Mandana Karboni ◽

...

Keyword(s):

Solid Lipid Nanoparticles ◽

Drug Loading ◽

Spherical Shape ◽

Lipid Nanoparticles ◽

Male Rats ◽

Scanning Calorimetry ◽

Solid Lipid ◽

Loading Efficiency

Purpose: To overcome side effects of repetitive administration of Diazepam (Dzp) besides gaining benefits from sustaining release (SR) of the drug, which contributes to patient compliance, we concentrated on designing and preparing Dzp Solid Lipid Nanoparticles (SLNs). Methods: Using cholesterol (CHOL), stearic acid (SA) and glycerol monostearate (GMS), SLNs were prepared by high shear homogenization technique coupled with sonication. Polysorbate 80 (Tween 80) was used as a nonionic surfactant. After modification of prepared SLNs, particle size, zeta potential, drug-loading efficiency, morphology and scanning calorimetry as well as release studies were conducted. To increase the stability of desired particles, freeze-drying by cryoprotectant was carried out. In the final stage, In-vivo study was performed by oral (PO) and intraperitoneal (IP) administration to Wistar male rats. Results: Results indicated that optimized prepared particles were in average 150 nm diameter in spherical shape with 79.06 % loading efficiency and release of more than 85% of loaded drug in 24 hours. In-vivo investigations also illustrated differences in blood distribution of Dzp after loading this drug into SLNs. Conclusion: Based on the findings, it seems that drug delivery using SLNs could be an opportunity for solving complications of Dzp therapy in future.

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Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2019.12.2.5 ◽

2020 ◽

Vol 12 (2) ◽

pp. 4474-4491

Author(s):

Rajkumar Aland ◽

Ganesan M ◽

P. Rajeswara Rao ◽

Bhikshapathi D. V. R. N.

Keyword(s):

Particle Size ◽

Drug Release ◽

Solid Lipid Nanoparticles ◽

Drug Loading ◽

Entrapment Efficiency ◽

Lipid Nanoparticles ◽

Tem Analysis ◽

In Vitro Drug Release ◽

Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements. In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

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A promising dual-drug targeted delivery system in cancer therapy: nanocomplexes of folate–apoferritin-conjugated cationic solid lipid nanoparticles

Pharmaceutical Development and Technology ◽

10.1080/10837450.2021.1920037 ◽

2021 ◽

pp. 1-9

Author(s):

Abbas Amer Ridha ◽

Soheila Kashanian ◽

Ronak Rafipour ◽

Abbas Hemati Azandaryani ◽

Hossein Zhaleh ◽

...

Keyword(s):

Cancer Therapy ◽

Delivery System ◽

Targeted Delivery ◽

Solid Lipid Nanoparticles ◽

Lipid Nanoparticles ◽

Solid Lipid ◽

Targeted Delivery System ◽

Dual Drug

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Positive-charged solid lipid nanoparticles as paclitaxel drug delivery system in glioblastoma treatment

European Journal of Pharmaceutics and Biopharmaceutics ◽

10.1016/j.ejpb.2014.10.017 ◽

2014 ◽

Vol 88 (3) ◽

pp. 746-758 ◽

Cited By ~ 39

Author(s):

Daniela Chirio ◽

Marina Gallarate ◽

Elena Peira ◽

Luigi Battaglia ◽

Elisabetta Muntoni ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Solid Lipid Nanoparticles ◽

Lipid Nanoparticles ◽

Solid Lipid

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Tamoxifen Drug Loading Solid Lipid Nanoparticles Prepared by Hot High Pressure Homogenization Techniques

American Journal of Pharmacology and Toxicology ◽

10.3844/ajptsp.2008.219.224 ◽

2008 ◽

Vol 3 (3) ◽

pp. 219-224 ◽

Cited By ~ 33

Author(s):

Nagi A. ALHaj ◽

Rasedee Abdullah ◽

Siddig Ibrahim ◽

Ahmad Bustamam

Keyword(s):

High Pressure ◽

Solid Lipid Nanoparticles ◽

Drug Loading ◽

Lipid Nanoparticles ◽

High Pressure Homogenization ◽

Solid Lipid

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Development of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers of Loteprednol Etabonate: Physicochemical Characterization and Ex Vivo Permeation Studies

10.21203/rs.3.rs-1145116/v1 ◽

2021 ◽

Author(s):

Burcu Üner ◽

Samet Özdemir ◽

Çetin Taş ◽

Yıldız Özsoy ◽

Melike Üner

Keyword(s):

Particle Size ◽

Solid Lipid Nanoparticles ◽

Drug Loading ◽

Physicochemical Characterization ◽

Lipid Nanoparticles ◽

Nanostructured Lipid Carriers ◽

Fickian Diffusion ◽

Control Group ◽

Loteprednol Etabonate ◽

Solid Lipid

Abstract Purpose Loteprednol etabonate (LE) is a new generation corticosteroid that is used for the treatment of inflammatory and allergic conditions of the eye, and management of seasonal allergic rhinitis nasally. LE which is a poorly soluble drug with insufficient bioavailability, has a high binding affinity to steroid receptors. Sophisticated colloidal drug delivery systems of LE could present an alternative for treatment of inflammatory and allergic conditions of the skin. For this purpose, solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were attempted to improve for transdermal LE delivery for the first time. Methods SLN and NLC were produced by hot homogenization and ultrasonication technique. Formulations were characterized by dynamic light scattering, scanning electron microscopy, fourier transform infrared spectroscopy and differential scanning calorimetry. Their physical stability was monitored for 3 months of storage. Drug release profiles and permeation properties of SLN and NLC through the porcine skin were investigated. Results It was determined that SLN and NLC below 150 nm particle size had a homogeneous particle size distribution as well as high drug loading capacities. They were found to be stable both physically and chemically at room temperature for 90 days. In terms of release kinetics, it was determined that they released from SLN and NLC in accordance with Fickian diffusion release. Formulations prepared in this study were seen to significantly increase drug penetration through pig skin compared to the control group (p ≤ 0.05). Conclusion SLN and NLC formulations of LE can be stated among the systems that can be an alternative to conventional systems with less side-effect profile in the treatment of inflammatory problems on the skin.

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