A brief review on solid lipid nanoparticles: part and parcel of contemporary drug delivery systems

Drug delivery technology has a wide spectrum, which is continuously being upgraded at a stupendous speed. Different fabricated nanoparticles and drugs possessing low solubility and poor pharmacokinetic profiles are the two major substances extensively delivered to target sites. Among the colloidal carriers, nanolipid dispersions (liposomes, deformable liposomes, virosomes, ethosomes, and solid lipid nanoparticles) are ideal delivery systems with the advantages of biodegradation and nontoxicity. Among them, nano-structured lipid carriers and solid lipid nanoparticles (SLNs) are dominant, which can be modified to exhibit various advantages, compared to liposomes and polymeric nanoparticles. Nano-structured lipid carriers and SLNs are non-biotoxic since they are biodegradable. Besides, they are highly stable. Their (nano-structured lipid carriers and SLNs) morphology, structural characteristics, ingredients used for preparation, techniques for their production, and characterization using various methods are discussed in this review. Also, although nano-structured lipid carriers and SLNs are based on lipids and surfactants, the effect of these two matrixes to build excipients is also discussed together with their pharmacological significance with novel theranostic approaches, stability and storage.

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or continue reading here: A brief review on solid lipid nanoparticles: part and parcel of contemporary drug delivery systems – Yongtao Duan, Abhishek Dhar, Chetan Patel, Mehul Khimani, Swarnali Neogi, Prolay Sharma, Nadavala Siva Kumar and Rohit L. Vekariya – DOI: 10.1039/D0RA03491F (Review Article) RSC Adv., 2020, 10, 26777-26791


Principle of lipid nanoparticle formulation

General ingredients

SLNs are comprised of a phospholipid-coated solid hydrophobic core matrix (containing the hydrophobic tails of the phospholipid section) (Fig. 2). Also, SLNs consist mainly of solid lipid(s), emulsifiers together with APIs such as drugs, genes, DNA, plasmid, and proteins. The lipids utilized in the formation of SLNs are surfactant stabilized, and thus solid at both physiological and room temperature. Depending on their structure, lipids are mainly divided into fatty acids, fatty esters, fatty alcohols, triglycerides, and partial glycerides. Ionic and nonionic polymers (Pluronic® such as F-68 and F127), surfactants, and organic salts are used as emulsifiers. However, their physicochemical characteristics also affect the behavior of the corresponding SLNs in both in vivo and in vitro release. The formation of colloidal nanoparticles depends on the interfacial tension and surface tension between two liquids. Thus, the main principle for the formation of solid lipid nanoparticles is the adhesive forces between two liquids. Normally, the interfacial tension between two liquids is less than their surface tension because of the weaker adhesive forces compared to that with gas. Molecules at the interface constitute surface free energy of interfacial tension, while they undergo agitation and form a spherical system to minimize the surface free energy.

From the publication “A brief review on solid lipid nanoparticles: part and parcel of contemporary drug delivery systems” the interesting Table 2 SLN formulations reported by different researchers

DrugLipidSurfactant/emulsifierCo-SurfactantMethod for preparation of SLNs
Amphotericin BCompritol® ATO 888, Precirol ATO 5 and stearic acid,Pluronic® F-68, Pluronic® F-127,Solvent diffusion method
Compritol® ATO 888 (glycerylbehenate), glycerylpalmitostearate (Precirol® ATO 5), medium chain triglycerideTween 20, Pluronic® F-127, Cremophor RH40, polyoxyethylene (40) stearate (Myrj 52)HPHDLS, zeta potential, HPLC, TEM, FTIR, DSC, PXRD, 1H NMR90–260
BaclofenStearic acidEpikuron 200 (92% phosphatidylcholine)Propionic acid, butyric acid, and sodium taurocholateMultiple (w/o/w) warm, microemulsion
BuspironeHClCetyl alcohol, SpermacetiPluronic® F-68, Tween 80Emulsification-evaporation followed by ultrasonication
CamptothecinSoybean lecithin, stearic acidPluronic® F-68, Tween 80Glycerol, PEG 400, PPGHot HPH
CarvedilolStearic acidPluronic® F-68Sodium taurocholate and ethanolMicroemulsion
ClozapineTrimyristin, tripalmitin, tristearin, soy phosphatidylcholinePluronic® F-68Ultrasonication method
Crypto-TanshinoneGlycerylmonostearate, Compritol 888 ATOSoy lecithin, Tween 80, sodium dehydrocholateUltrasonic and high-pressure homogenization method
CurcuminCompritol 888 ATOSoy lecithin, Tween 80Microemulsion
TristearinPolyoxyethylene (10) stearyl ether (Brij®S10), polyoxyethylene (100) stearyl ether (Brij® S100)Oil-in-water emulsion techniquePCS, zeta potential111–350
Cyclosporine AImwitor® 900Tagat®S, sodium cholateHPH, hot HPH
DiazepamCompritol 888 ATO, Imwitor® 900Pluronic® F-68, Tween 80Ultrasound techniques modified high-shear homogenization and
Doxorubicin hydrochlorideGlycerylcapratePolyethylene glycol 660 hydrox-ystearate (Solutol®HS15)Ultrasonic homogenization
FenofibrateVitamin E TPGS, Vitamin E 6–100Hot HPH
HydrocortisonePrecirol® ATO 5, Compritol® 888 ATO, Rylo TM MG 14 Pharma, Dynasan® 114 Dynasan® 118, Tegin® 4100Tween 80Hot high pressure homogenization
IbuprofenTrilaurin, tripalmitin, stearic acidPluronic®F127, sodium taurocholateSolvent-free high-pressure homogenization (HPH)
IdarubicinStearic acidEpikuron 200 (soy phosphatidylcholine 95%)Taurocholate sodium saltMicroemulsion
Emulsifying waxPolyoxyl 20-stearyl ether (Brij 78), D-alpha-tocopheryl polyethylene glycol succinate (vitamin E TPGS),DSPE-PEG3000Sodium taurodeoxycholate (STDC), sodium tetradecylsulfate (STS)PCS, Zetasizer nano Z94.4 (blank), 80–104 (loaded sample)
KetoprofenBeeswax and carnauba waxTween 80, egg lecithinMicroemulsion technique
LopinavirCompritol 888 ATO (glycerylbehenate)Pluronic®F127Hot homogenization, ultrasonication
LovastatinTriglyceride, and phosphatidylcholine 95%Pluronic®F68Hot homogenization ultrasonication
MethotrexateStearic acid, monostearin, tristearin, and Compritol 888 ATOL-α-Soya lecithin, and Sephadex G-50Solvent diffusion method
NevirapineSteric acid, Compritol 888 ATODimethyldioctadecyl ammonium bromide (DODAB), Tween 80, Lecithin1-ButanolMicroemulsion
Nitrendipinetriglyceride and phosphatidylcholinePluronic®F68Hot homogenization ultrasonication method
Octadecylamine-fluorescein isothiocyanateStearic acidOtcadecylamine, polyethylene glycol monostearate (PEG2000-SA)Solvent diffusion
PentoxifyllineStearic acid, cetyl alcohol, soy lecithin,Tween 20, Pluronic F®68Homogenization followed by the ultrasonication
PraziquantelHydrogenated castor oilPoly vinyl alcohol (PVA)Hot homogenization and ultrasonication
PuerarinMonostearin, and soy lecithinPluronic F®68Solvent injection method
QuercetinGlycerylmonostearat, soy lecithinTween-80 and PEG 400Emulsification-solidification
RifampicinStearic acidPVAEmulsion-solvent diffusion
TobramycinStearic acidEpikuron 200Sodium taurocholateMicroemulsion
VinpocetineGlycerylmonostearat, soy lecithin, polyoxyethylene hydrogenated castor oilTween 80Ultrasonic-solvent emulsification
As per Table 2 SLN formulations reported by different researchers of "A brief review on solid lipid nanoparticles: part and parcel of contemporary drug delivery systems"
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