Loaded Nanostructured Lipid Carriers Research Articles

Design and Development of Valsartan Loaded Nanostructured Lipid Carrier for the Treatment of Diabetic wound Healing

Diabetes mellitus is a group of metabolic diseases identified by hyper glycaemia that results from defects in insulin secretion, insulin action or both. It can also be referred as metabolic disorder. The main objective of this research is to enhance the protection of wound healing from the valsartan loaded Nanostructure Lipid carrier. Valsartan is the angiotensin II antagonist drug, which is of BCS class II category. Nanostructure lipid carrier is a colloidal carrier system which is having many advantages such as improvement in Bioavailability, Increase in the solubility and therapeutic efficacy. The prepared Nanostructure lipid carrier was consisting of palmitic acid as solid lipid and soya oil as liquid lipid were prepared by melt emulsification method. Optimization and Characterization of Valsartan loaded NLCs have been done by DSC, FT-IR, Particle size, Zeta potential, Scanning Electron microscopy, Stability study, Entrapment efficiency, Release kinetics and In-vitro drug release studies. The In-vivo have also been done for the treatment of Diabetic wound healing. In Conclusion, it is shown that the valsartan loaded Nanostructure lipid carrier formulation was very effectively for the treatment of Diabetic wound Healing.

Development of Pranoprofen Loaded Nanostructured Lipid Carriers to Improve Its Release and Therapeutic Efficacy in Skin Inflammatory Disorders

Pranoprofen (PF)-loaded nanostructured lipid carriers (NLCs), prepared using a high-pressure homogenization method, have been optimized and characterized to improve the biopharmaceutical profile of the drug. The optimized PF-NLCs exhibited physicochemical characteristics and morphological properties that were suitable for dermal application. Stability assays revealed good physical stability, and the release behavior of PF from these NLCs showed a sustained release pattern. Cell viability results revealed no toxicity. Ex vivo human skin permeation studies in Franz diffusion cells were performed to determine the influence of different skin penetration enhancers (pyrrolidone, decanol, octanoic acid, nonane, menthone, squalene, linoleic acid, and cineol) on skin penetration and retention of PF, being the highest dermal retention in the presence of linoleic acid. The selected formulations of NLCs exhibited a high retained amount of PF in the skin and no systemic effects. In vivo mice anti-inflammatory efficacy studies showed a significant reduction in dermal oedema. NLCs containing linoleic acid presented better anti-inflammatory efficacy by decreasing the production of interleukins in keratinocytes and monocytes. The biomechanical properties of skin revealed an occlusive effect and no hydration power. No signs of skin irritancy in vivo were detected. According to these results, dermal PF-NLCs could be an effective system for the delivery and controlled release of PF, improving its dermal retention, with reduced dermal oedema as a possible effect of this drug.

Fabrication and Characterization of Timolol Maleate and Brinzolamide Loaded Nanostructured Lipid Carrier System for Ocular Drug Delivery.

The combination of timolol maleate (TM) and brinzolamide (BRZ) has potential therapeutic prospects for treating glaucoma. However, the conventional formulation of TM and BRZ exhibits sub optimal therapeutic effects attributable to the poor ocular bioavailability of these drugs. Therefore, the aim of the present study was to design and evaluate TM and BRZ loaded nanostructured lipid carrier (NLC) to enhance the bioavailabilities, permeation and precorneal residence time of these drugs that would result in efficacious treatment of glaucoma. In this study, combination of drugs with different characteristic properties was loaded in NLC. The dual drugs loaded NLC was prepared by melt emulsification technique and evaluated for characteristic properties such as particle size (PS), polydispersity index (PDI), entrapment efficiency (EE) and drug loading (DL), in vitro drug release and ex vivo drug penetration studies. The PS and PDI of optimized NLC formulation were found to be 110.36 ±0.47 nm and 0.24 ± 0.00 respectively. The EE and DL of optimized NLC formulation were found to be 77.12 ± 0.64 % and 0.360 ± 0.01 % for TM respectively; whereas, 70.73±0.64 % and 0.71 ± 0.02 %for BRZ respectively. In vitro drug release studies showed a comparable initial rapid release of around 34 ± 2.90 % for TM and 38 ± 3.10 % for BRZ in the first 5 h followed by sustained drug release around 72.29 ± 5.90 % for TM and 70.08 ± 6.40 % for BRZ until last 24 h. Ex vivo drug penetration studies showed about 33.47 ± 2.80 % of TM and 36.20 ± 2.80 % of BRZ permeated in the first 5 h followed by 72.30 ± 6.40% of TM and 67.69 ± 6.500 % of BRZ until 24 h. There was remarkable enhancement in the release pattern and permeation of both the drugs from NLC as compared to that from their suspension. With dextrous optimization of dose and excipients concentration, the dual drugs with different characteristic properties can be successfully loaded in NLC formulation.

Development of γ-Oryzanol Rich Extract from Leum Pua Glutinous Rice Bran Loaded Nanostructured Lipid Carriers for Topical Delivery.

Leum Pua is native Thai glutinous rice that contains antioxidants higher than white rice and other colored rice. One of the major antioxidants in rice brans is γ-oryzanol (GO). In this study, Leum Pua glutinous rice bran was extracted by different solvents. Oleic acid (~40 g/100 g extract), linoleic acid (~30 g/100 g extract), and palmitic acid (~20 g/100 g extract) were found to be major lipid components in the extracts. Methanol extract showed less variety of lipid components compared to the others. However, hexane extract showed the highest percent of γ-oryzanol compared to other solvents. Therefore, the hexane extract was selected to prepare nanostructured lipid carriers (NLC). The prepared NLC had small particles in the size range of 142.9 ± 0.4 nm for extract-loaded NLC and 137.1 ± 0.5 nm for GO-loaded NLC with narrow size distribution (PI < 0.1) in both formulations. The release profile of extract-loaded NLC formulation was slightly higher than GO-loaded NLC formulation. However, they did not follow the Higuchi model because of small amounts of γ-oryzanol loaded in NLC particles.

Design, Development and Invivo Pharmacokinetic Evaluation of Cardiovascular Drug Loaded Nano Structured Lipid Carrier System

The Present investigation is to design, develop and optimize the Nanostructured Lipid Carrier (NLC) containing cardiovascular drug by various independent variables like formulation variables (concentration of phospholipids, surfactants, co-surfactant) and process variables (homogenization time and ultrasonication time). The objective of this research is to choose the suitable and reproducible technique for the formulation of NLC based on dependent variables like Particle Size (PS) in nm, Polydispersity Index (PDI), Zeta potential (ZP) in mV and Entrapment efficiency (EE%) by applying Box Behnken design utilizing - Multiple linear regression method (Design expert 9 software, stat-ease, Inc. USA) and another objective is to prove the enhancement of bioavailability of drug in developed NLC. Comparative invivo pharmacokinetic studies was carried out to determine AUC, Cmax, Tmax , Ke, Vd between drug loaded NLC and commercially available dosage form to prove the enhancement of bioavailability in NLC. From the results obtained, it was concluded that hot homogenization was an optimized technique for the preparation of NLC containing carvedilol and NLC shows better bioavailability when compare to commercial formulation. This data was related to the research project sanctioned by Department of science and technology (DST) entitled “Development of Lipid Nanoparticles Enriched Hydrogels for Transdermal Drug Delivery: Formulation, In vitro Characterization and Pharmacodynamic studies in Animals”

Tretinoin Loaded Nanostructured Lipid Carrier (NLC): Safe and Effective Drug Delivery System

Background and Aim: Tretinoin has been formulated in different vehicles in an attempt to decrease the irritation associated with the past formulations. So to improve the skin uptake and reduce irritation of tretinoin, we need a carrier with an ability of skin targeting. For achieving this purpose, nanostructured lipid carriers (NLCs) are chosen as a new topical drug delivery system to improve the absorption and reduce side effects. Keywords: Tretinoin, nanostructured lipid carriers, high pressure homogenizer, safety, atomic force microscopy, morphology.

Inducing Optimal Antitumor Immune Response through Coadministering iRGD with Pirarubicin Loaded Nanostructured Lipid Carriers for Breast Cancer Therapy.

Chemotherapeutic agents trigger antitumor immune response through inducing immunogenic tumor cell death. However, severe toxicity to immune system and insufficient immunogenic cell death hinder chemotherapy from arousing efficient antitumor immunity in vivo. In this study, the cytotoxic drug, pirarubicin (THP), was entrapped into nanostructured lipid carriers (NLC); THP-NLC significantly reduced the toxicity of THP to immune system and improved immune status of breast cancer bearing mice. When THP-NLC was coinjected with iRGD (a tumor-penetrating peptide), drug accumulation in tumors was greatly elevated, which led to significant control of tumor growth and increase of immunogenic tumor cell death. Subsequently, the cytotoxic T lymphocytes (CD3+ and CD8+ cells) infiltration and cytokine (IFN-γ and INF-α) secretion in tumors were heavily increased. The efficient T-cell dependent control of tumors in the late stage and the lower side effects contributed to the longest whole survival of THP-NLC + iRGD treated mice. Therefore, the coadministration of THP-NLC with iRGD resulted in increased tumor cell direct-killing death and enhanced antitumor immune response. Our results illustrated that THP could serve as an immunogenic cell death inducer and the proposed drug delivery strategy might impact cancer immunotherapy by arousing increased immunogenic tumor cell death.

Quality by Design (QbD)-enabled development of aceclofenac loaded-nano structured lipid carriers (NLCs): An improved dermatokinetic profile for inflammatory disorder(s)

Present study was designed to prepare and characterize aceclofenac loaded nanostructured lipid carriers (NLCs) employing Quality by Design (QbD)-oriented approach. The NLCs were evaluated for their transdermal penetration potential and stability. Aceclofenac loaded nanostructured lipid carriers (NLCs) were prepared & characterized, by employing Quality by Design (QbD)-oriented approach and further evaluated for transdermal penetration potential and stability. Different lipids and surfactants were chosen to prepare NLCs using microemulsion method as critical material attributes (CMAs). A 33 factorial design was used for optimization of NLCs, and evaluating them for different critical quality attributes (CQAs), viz. particle size, polydispersity index (PDI), zeta potential, in vitro drug release, entrapment efficiency. The effect of CMAs such as lipids, oil: lipid ratio and concentration of surfactants on CQAs viz. drug entrapment efficiency and particle size were systematically evaluated to optimize NLCs. The optimized NLCs were further incorporated into carbopol gel and characterized for texture and rheology profile followed by in vitro and in vivo evaluations. The optimized ACE-NLCs were found to be spherical, nanometric in size with higher drug loading and entrapment efficiency. Results of the in vitro drug release study showed that the developed formulation followed Korsmeyer-Peppas model showing Fickian diffusion. The release was biphasic i.e., initial burst release followed by sustained drug release upto 48h. The optimized NLCs-based gel formulation showed superior texture, rheological profile and showed better cell uptake efficiency on hyperkeratinocytic cells (HaCaT cell lines) with higher ex vivo skin permeability efficiency vis-à-vis marketed formulation. In conclusion, dermatokinetic modeling and pharmacodynamic study using carrageenan induced edema mice suggests that aceclofenac loaded NLCs hydrogel may provide a better delivery alternative to target various skin layers.

Nebivolol Hydrochloride Loaded Nanostructured Lipid Carriers as Transdermal Delivery System: Part 1: Preparation, Characterization and In Vitro Evaluation

Nebivolol hydrochloride (NEB) is a 3rd generation highly selective β1-blocker with antihypertensive properties, the elimination half-life is about 10 hrs and the oral bioavailability is about 12%.&#x0D; The study was aimed to develop nanostructured lipid carriers (NLC) for transdermal delivery of NEB.&#x0D; The study involves two separate parts, part 1 (current) involves preparation and characterization of NEB loaded NLCs (NEB-NLCs). Part 2 of the study, NEB-NLCs based gel was formulated using gelling agent carbapol 934 as transdermal delivery system using rat skin. Part 2 of the study will be presented separately in the forthcoming issue.&#x0D; The current investigation describes the effect of type and concentration of different solid lipids, liquid lipids, and surfactant/co-surfactant on the characteristics of NLC such as particle size, polydispersity index, zeta potential, drug entrapment efficiency, and drug release profile. Transmission electron microscopy, scanning electron microscope and atomic force microscope revealed nearly spherical shape NLC with negligible effect of liquid lipid (oleic acid) content on the particle morphology. The differential scanning calorimetry demonstrated depression in the melting point and crystallinity index of the NLCs with increasing the amount of liquid lipid. The in vitro drug release studies demonstrated that 93% of the drug was released over 24hrs. The NEB-NLCs possessed a biphasic release pattern characterized by a rapid initial release followed by a sustained release.

Development of Piroxicam Loaded Nanostructured Lipid Carriers for Spondylitis Treatment

Development of Piroxicam Loaded Nanostructured Lipid Carriers for Spondylitis Treatment

Preparation and Characterization of Broad-Spectrum Sunscreens Loaded Nanostructured Lipid Carrier

A comprehensive photoprotective formulation was developed to enhance photoprotection ,compared to a conventional nanoemulsion ,having the concentration of two new molecular sunscreens, namely Diethylamino hydyoxybenzoyl hexyl benzoate(Uvinul ® A Plus) and Ethylhexyl triazone(Uvinul® T 150). In the present paper, the sunscreen mixture was incorporated into nanostructured lipid carriers (NLCs). After the production by hot high pressure homogenization, the NLC were analyzed in terms of particle size, physical state, particle shape, ultraviolet absorbance and stability. The particle size for all NLC was around 100-900 nm after production. The determination of 2 organic UV filters was performed by HPLC with UV spectrophotometric detection. The loading capacities for molecular sunscreens was up to 30%. In the sunlight, the retention rate of Uvinul ® A Plus and Uvinul ® T150 was still up to 80% after three months .

Investigation of Tacrolimus Loaded Nanostructured Lipid Carriers for Topical Drug Delivery

The objective of this investigation was to develop nanostructured lipid carriers (NLCs) of tacrolimus by the hot homogenization technique by sonication. NLCs are commonly prepared by emulsification and lyophilization. The feasibility of fabricating tacrolimus-loaded NLCs was successfully demonstrated in this study. The developed NLCs were characterized in terms of their particle size, zeta potential, entrapment efficiency (EE) of tacrolimus, and morphology. Studies were conducted to evaluate the effectiveness of the NLCs in improving the penetration rate through hairless mouse skin. Tacrolimus-loaded NLCs were found to have an average size of , a zeta potential of , and an EE of 50%. In vitro penetration tests revealed that the tacrolimus-loaded NLCs have a penetration rate that is 1.64 times that of the commercial tacrolimus ointment, Protopic.