Effect of polymer charge on the formation and stability of anti-inflammatory drug loaded nanostructured lipid carriers: physicochemical approach

Abstract

Proposed model of NSAID loaded and polymer coated NLC alongwith its dependence of size ( ), PDI ( ), release rate ( ) and absorption maxima ( ) as well as its morphology and antibacterial activity ARTICLE This journal is Nanostructured lipid carriers (NLCs), with potential drug delivery capabilities, were formulated using soylecthin (SLC), tristearin (TS) and palmitic acid (PA) in the absence and the presence of two antiinflammatory drugs, diclofenac sodium (DNa) and indomethacin (IMC). Tween 60 was used as stabilizer separetely in combination with sodium carboxymethyl cellulose (NaCMC, anionic), polyethylene glycol (PEG, nonionic) and N, N, dimethyl-N-dodecyl derivative of hydroxyethyl cellulose (LM200, cationic). Both DNa and IMC substantially decreased size and increased polydispersity index (PDI) of the NLCs. Hydrodynamic parameter, viz., size, zeta potential and polydispersity index as well as the thermal behaviour of the NLCs depended on the type and charge of the added polymers. Weak interactions between drug and lipid matrices in the bulk mixtures were established through FT-IR studies. NLC formulations exhibited lower entrapment efficiency and loading content in case of DNa compared to IMC due to the higher ionic nature of the former drug. Polymers influenced the entrapment efficiency and loading ability of the NLCs in case of both DNa and IMC. 85% of the entrapped DNa was released from the NLC, compared to 54% release in case of IMC; the drug release rate were higher for PEG and NaCMC coated systems. LM200 delayed the drug release process with respect to NaCMC and PEG. Both DNa and IMC loaded NLCs inhibited the growth of gram positive bacteria, Bacillus amyloliquefaciens. It was concluded that the physicochemical properties of NLCs could effectively be modified by using polymers; thus the biomimetic characteristics of lipids and architectural advantage of polymers can be combined to yield a superior drug delivery system.

Physicochemical Characterization of Chrysin‐Derivative‐Loaded Nanostructured Lipid Carriers with Special Reference to Anticancer Activity

“…NLC were prepared using hot homogenization followed by ultrasonication according to our previous works (Karmakar et al, ; Nahak et al, ; Sapkota et al, ). In the NLC formulation, CP and TP were used in equimolar ratio, whereas the quantity of OA was varied from 10 to 30 mol% in steps of 10 mol%.…”

“…The supernatant was collected and analyzed colorimetrically for the estimation of the free drug. EE and DL were calculated as (Karmakar et al, ; Nahak et al, ; Sapkota et al, ) follows: where W total CHR , W free CHR , and W total lipid represent the total amount of drug, free drug present in the dispersion medium, and the total amount of lipid in the NLC formulation, respectively.…”

“…They are also known as modified solid lipid nanoparticles (SLN). They are nanocolloidal suspensions in the size range 10–1000 nm (Karmakar et al, ; Nahak et al, ; Sapkota et al, ). The major difference between SLN and NLC lies in the choice of the lipid blends.…”

“…While symmetric hydrocarbon‐chain‐containing lipid components are used for the preparation of SLN, two or more structurally different lipids (solid and/or liquid) are used for NLC. NLC have superiority over the other drug delivery systems such as liposomes, nanoemulsions, microemulsions, nanocapsules, nanosponges, and polymeric nanoparticles (Karmakar et al, ; Nahak et al, ; Sapkota et al, ; Yadav et al, ). Superior pharmaceutical loading capacity, possibility of specific targeting, and sustained‐release characteristics over other drug delivery systems make NLC superior.…”

Effects of Fatty Acids on the Interfacial and Solution Behavior of Mixed Lipidic Aggregates Called Solid Lipid Nanoparticles

“…Further details are available in our recent publications 14,15 . SLN suspensions were stored at 4 in the dark.…”