Nanocarrier Technologies for Enhancing the Solubility and Dissolution Rate of Api
Debarshi Kar Mahapatra, Sanjay Kumar Bharti in Medicinal Chemistry with Pharmaceutical Product Development, 2019
These are biocompatible, biodegradable lipids which are solid at room and body temperature. The lipids can be used within the range of 5–40%. Examples include: Triglycerides (trimyristin, tripalmitin, tristearin).Polymers like soya phosphatidyl choline, PLGA, sodium alginate, chitosan, etc.Glyceryl monostearate (GMS) (Imwitor® 900).Glyceryl behenate (Compritol® 888 ATO, GeleolTM).Glyceryl palmitostearate (Precirol® ATO 5).Wax (cetyl palmitate).
Innovative Delivery Systems for Andrographolide Delivery
Madhu Gupta, Durgesh Nandini Chauhan, Vikas Sharma, Nagendra Singh Chauhan in Novel Drug Delivery Systems for Phytoconstituents, 2020
Solid lipid nanoparticles (SLNs) consist of colloidal carriers constituted by lipids and stabilized by surfactants, whose lipid matrix is solid at room temperature. As a drug carrier, those structures protect encapsulated drugs against degradation as well as provide controlled drug delivery. SLNs’ average particle size varies from 10 to 1000 nm (Wissing et al., 2004). The lipid matrix selections are biocompatible and biodegradable, decreasing the risk of acute and chronic toxicity (Pawar et al., 2016). Usually, the used lipids in SLN matrices are biocompatible triglycerides, including trimyristin (tri-C14), tripalmitin (tri-C16), and tristearin (tri-C18); simple esters, as glyceryl monostearate or glyceryl behenate; as well as fatty acids, like stearic acid (Wissing et al., 2004). Other advantages of these novel drug delivery systems include their long-term stability, ability to enhance the encapsulated drug bioavailability, possibility to control and target drug release, versatility, and formulation efficiency due to the advantageous capability of encapsulating both lipophilic and hydrophilic drugs (Wissing et al., 2004).
Historical Background
Margit Hamosh in Lingual and Gastric Lipases: Their Role in Fat Digestion, 2020
Most important was the fact that he recognized that the fats found in the bodies of different species were all composed of fatty acids and that the difference between the properties of human fat and mutton tallow was the result of mixtures of fatty acids of different melting points.3 For the discussion in the following chapters of this book it is important to point out that his interest in short-chain fatty acids was related to their possible effect on the palatability of foods.3 In spite of the marked progress in the chemistry of fats, and although Berthelot suggested the possible existence of mixed triglycerides in 1860, it was generally assumed until the very end of the last century that natural fats consist of mixtures of simple glycerides.8 In 1897, Heise demonstrated the presence of oleodistearin in the fat from a member of the genus Allanblackia.9 The essentially mixed character of the glycerides of natural fats was further documented by the studies of Bomer and colleagues.10, 11 While the early studies accomplished the separation of glycerides by fractional crystallization,8 Krafft used fractional distillation under reduced pressure to isolate trilaurin from laurel kernel fat and trimyristin from nutmeg butter.12
Ameliorating the in vivo antimalarial efficacy of artemether using nanostructured lipid carriers
Published in Journal of Microencapsulation, 2018
Ravisankar Vanka, Gowthamarajan Kuppusamy, Simhadri Praveen Kumar, Uday Krishna Baruah, Veera Venkata Satyanarayana Reddy Karri, Vimal Pandey, Phanithi Prakash Babu
The selection criterion for solid lipid and liquid lipids depends on their ability to solubilise ARM as the solubility of the drug in the solid lipid is one of the major concerns that influences the drug entrapment efficiency and in vitro drug release. So we adopted affinity study method as described previously (Negi et al., 2014). Preliminary solubility studies with solid lipids demonstrated that trimyristin had a good solubility (68.65 ± 7.72%) for ARM (Table 1). Further, Partition coefficient studies revealed that ARM had higher partitioning in trimyristin (82.71 ± 6.89) as compared to other lipids such as tristearin (72.89 ± 7.53), tripalmitin (49.95 ± 5.81), compritol 888 ATO (45.61 ± 4.69) and GMS (25.26 ± 9.87). This finding also correlated with the high solubility of the drug in trimyristin. Hence, trimyristin was selected as the solid lipid for the preparation NLCs. Among the liquid lipids for ARM, highest solubility was observed for capmul MCM (72 ± 1.23 mg/ml). Hence, capmul MCM as a liquid lipid was chosen for the preparation of NLCs. The result of the study showed good compatibility between trimyristin with capmul MCM without any phase separation of the congealed mass at a ratio of 70:30. Surfactant plays an important role in stabilisation of nanoparticles. Among the surfactants used, polysorbate 80 at 2% w/v (Table 1) showed highest solubility (22 ± 1.56 mg/ml) for ARM followed by polysorbate 20 (10 ± 2.94 mg/ml). The solubility studies revealed that trimyristin (solid lipid), capmul MCM (liquid lipid) and polysorbate 80 (surfactant) have high solubilising potential for ARM. Hence they are selected for the formulation of NLCs.
Development and characterization of cationic solid lipid nanoparticles for co-delivery of pemetrexed and miR-21 antisense oligonucleotide to glioblastoma cells
Published in Drug Development and Industrial Pharmacy, 2018
Berrin Küçüktürkmen, Asuman Bozkır
The SLN formulation that has the smallest particle size (182.5 ± 2.5) and polydispersity index (0.260 ± 0.014) was prepared again by adding the active substance. After addition of the pemetrexed, particle size and polydispersity index were increased to 204.4 ± 5.5 nm and 0.430 ± 0.040, respectively. SLN formulations with a particle size of less than 200 nm remain longer in the blood stream, increase the duration of contact with the blood brain barrier, and enhance brain penetration of the drugs [9]. It is aimed to prepare SLN formulation with high encapsulation efficiency and small particle size. For this purpose, pemetrexed loaded SLNs were prepared using different solid lipids such as stearic acid, glyceryl tripalmitate and trimyristin. When stearic acid was used as lipid, nano size could not be obtained. Xie et al. [34] also found that SLNs prepared with stearic acid had a larger size and size distribution. This is associated with high viscosity and melting point of stearic acid. It has been noted that higher melting points of lipids may lead to less efficient homogenization, thereby leading to larger particle size and size distribution. The SLN formulation prepared using glyceryl tripalmitate had a particle size of 385.6 ± 21.5 nm. The smallest particle size (118.0 ± 0.9 nm) was obtained with using trimyristin. For this reason, formulation studies have been continued using trimyristin as a solid lipid. Encapsulation efficiency of F1 formulation prepared with trimyristin 1% and tween 80 1% was found 22.9 ± 0.2%. When the ratio of Tween 80 was increased to 2% (F2), increase in the encapsulation efficiency of pemetrexed to 32.1 ± 6.3% was observed (Table 2).
Comparative study of nisoldipine-loaded nanostructured lipid carriers and solid lipid nanoparticles for oral delivery: preparation, characterization, permeation and pharmacokinetic evaluation
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2018
Narendar Dudhipala, Karthik Yadav Janga, Thirupathi Gorre
ND was gifted sample from Orchid Labs (Chennai, India). Trimyristin (dynasan-114; glyceryl trimyristate) was purchased from Sigma-Aldrich Chemicals (Bangalore, India). Oleic acid and dialysis membrane (70 dm) were purchased from Himedia Chemicals (Hyderabad, India). Egg lecithin E-80 was a gift sample from Lipoid (Germany). Poloxamer-188 was a gift sample from Dr. Reddy’s Labs (Hyderabad, India). Methanol, acetonitrile and chloroform of high-performance liquid chromatography (HPLC) grade were purchased from Merck, Mumbai, India. Centrisart filters (molecular weight cut-off 20,000 Da) were purchased from Sartorius (Goettingen, Germany).
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