Lipid Nano- and Microparticles: An Overview of Patent-Related Research

Table 4

Most important patents that concern the specific therapeutic/technological aims of lipid nano- and microparticles.

Therapeutic/technological aim	Patent number	Lipid particle type	Drug/active delivered	Brief description	Ref.
Cancer therapy	FR2935270	SLM	Temozolomide	Galenic form of SLM formulated with temozolomide in a lipid matrix	[127]
	WO2006128888	SLN	Cholesteryl butyrate, propionate	SLN, made up of cholesteryl butyrate and propionate as a lipid matrix, are used for the prevention and treatment of inflammatory pathologies	[128]
	US6685960	SLN		SLN, made up of cholesteryl butyrate and propionate as a lipid matrix, are used for tumor treatment	[129]
	WO2005092298	SLN	Platinum compounds	The loading of platinum derived compounds in SLN is obtained using a warm microemulsion method	[130]
	WO2004071498	LNC	P-glycoprotein inhibitor	LNC are stabilized by surfactants that can act as P-glycoprotein inhibitors and reduce tumor drug resistance	[131]
	CN200910065523	SLN	Cucurbitacin	A cucurbitacin-loaded SLN preparation method is disclosed, in which the formulation maintains its stability	[132]
	CN201110022618	PLN	Adriamycin	The loading of adriamycin into SLN is achieved via complexation with polyanion sodium alginate, leading to a sustained release formulation	[133]
	CN200810041865	SLN	Docetaxel	Long-circulating docetaxel-loaded SLN are formulated	[134]
	WO2014206093	SLN	Chinese herbal compound	The loading of Chinese herbal antitumor compounds into SLN significantly improves their bioavailability, reducing dosage and increasing therapeutic effects	[135]
	IN421/DEL/2008	SLN	Paclitaxel	Controlled delivery	[136]
Brain delivery	US2010247619	NLC	Riluzole	Medicinal formulations are prepared to treat amyotrophic lateral sclerosis and multiple sclerosis	[137]
	US6514519	SLN	Octadecyl-2-methyl-sn-glycero-3-phosphorylcholine (edelfosin)	SLN are loaded with edelfosin, which is suitable for the treatment of brain tumors and can also be administered orally	[138]
	WO9920256	SLN	—	BBB targeting of SLN is obtained via either specific protein linkages or absorption onto the SLN surface	[139]
	WO2011019954	SLN	—	SLN delivery to the brain is achieved via the perilymphatic fluid of the inner ear, through the cochlear aqueduct	[140]
	WO9927918	SLN	—	Small-sized SLN, obtained from warm microemulsions, can cross the BBB	[141]
	US20100129431	SLN	Idebenone	Injectable nanoparticles that are loaded with idebenone can protect from neuronal damage and improve recovery after brain trauma	[142]
	CN201610002634	SLN	Aripiprazole	Aripiprazole-loaded SLN for injection have high bioavailability, low toxic and side effects, and controlled-release targeting properties	[143]
	CN201610262638	SLN	Antidepressant composition	A mixture of curcumin, folic acid, lecithin, and HU-211 is loaded into SLN, with increased bioavailability	[144]
	IN201621034343	SLN	Tapentadol	In situ gel composition of loaded SLN for nose-to-brain delivery	[145]
	IN1251/MUM/2012	NLC	Ubidecarenone	Treatment of neurodegenerative disorders	[146]
	IN2009/MUM/2012	SLN	Granisetron	SLN-cyclodextrin complex for nose-to-brain delivery	[147]
	IN3451/DEL/2012	SLN	Carbidopa	Bionanoparticles and SLN to target the brain via administration through the ear cavity	[148]
Gene therapy	WO02051446	SLN	Nucleic acids	Cationic SLN are employed to condense nucleic acids on their surface	[149]
	WO2009051451	LDL-like	ASO, siRNA, and p-DNA	Cationic LDL-like nanoparticles can complex nucleic acids and be used to treat liver diseases	[150]
	WO2008096321	LNC	siRNA, p-DNA	A complex between a cationic lipid and a nucleic acid is loaded into the inner oily core of LNC	[151]
	WO2005120469	SLN	Anti-VEGF ASO	An anti-VEGF nucleotide is complexed with cationic SLN in order to inhibit angiogenesis, especially in the posterior segment of the eye	[152]
	WO2011015701	SLN	p-DNA	In order to achieve transfection, p-DNA is complexed with SLN that is functionalized with a cationic lipid or peptide, a nonionic surfactant, and a polysaccharide	[153]
	WO2017015552	SLN	siRNA	A solid lipophile siRNA cargo can be obtained using cationic SLN, a dextrin, and a sugar	[154]
	WO20040530056	SLN	p-DNA	A vaccine formulation is obtained by coating SLN with a nucleic acid that encodes for an immunogenic peptide, in the presence of a cholera toxin, used as an adjuvant	[155]
	IN201611003140	SLN	p-DNA, siRNA	Two-step process to entrap pDNA and siRNA within the lipid matrix of SLN	[156]
Protein and peptide delivery	WO9956733	SLN	Cyclosporine	When cyclosporine is loaded into SLN, a better pharmacokinetic profile, compared to commercial formulations, is obtained after oral administration	[157]
	CN201610203074	SLN	Sirolimus	Sirolimus-loaded SLN are employed as a nonirritant topical formulation for the treatment of multiple immune and inflammatory skin diseases (atopic dermatitis, eczema, dermatitis, lichen planus, psoriasis, vitiligo, rosacea, and sarcoidosis)	[158]
	WO2015007398	SLN	Antibody	Antibodies are loaded into SLN through hydrophobic ion pairing	[159]
	WO02051390	SLN	LHRH antagonist	LHRH-antagonist peptide is loaded into HPH-produced SLN	[160]
	WO2009080164	SLM	Growth hormone	Lipid-coated microparticles that are loaded with growth hormone are obtained by spray-drying, without denaturing the protein	[161]
	WO2010017965			Lipid-coated microparticles that are loaded with growth hormone are obtained by spray-drying and spray congealing, without denaturing the protein	[162]
	WO0071077	SLN	Antigen for vaccine	SLN are employed as stable and biocompatible adjuvants for vaccines	[163, 164]
	WO0071154
	WO2017097783			Aminoalkyl glucosaminide phosphate is employed as a vaccine adjuvant in antigen-complexed cationic SLN	[165]
	WO0164254	SLM		Antigen-loaded spray-dried SLM are functionalized with a ligand that is specific for antigen-presenting cells, inducing immune responses	[166]
	CN201010522545	SLN	Catalase	A two-step emulsion process from a multiple W/O/W emulsion is used to load catalase into SLN, greatly increasing the stability of the enzyme and prolonging its effective activity duration	[167]
	WO2007113665	PLN	Various therapeutic peptides	Lectin-functionalized PLN are loaded with therapeutic peptides in order to increase oral uptake and/or immunization	[168]
Antioxidant and vitamin delivery	WO2006102768	SLN	Tocopherol derivatives	A suitable SLN formulation is engineered with a tocopherol derivative in the lipid matrix and a water-soluble antibiotic in the aqueous phase	[169]
	WO2011028757	SLN, NLC	Tocotrienols	Lipid compositions that include tocotrienols are engineered	[170]
	WO2007103435	SLN, NLC	Curcuminoids	Curcuminoid formulations with enhanced bioavailability that are suitable for Alzheimer’s disease treatment are produced	[171]
	WO2010010431				[172]
	WO2013105026	SLN	Vitamins	SLN are employed as vehicles for vitamins, especially vitamin D and retinoic acid, with the aim of treating tuberculosis	[173]
	WO9505164	SLN	Ubidecarenone	Ubidecarenone-loaded SLN are engineered	[174]
	IN718/CHE/2013	SLN	Rutin	The treatment of diabetes and diabetic foot ulcers in the form of an oral drug, and the treatment of diabetic foot ulcers in the form of an ointment	[175]
	IN79/DEL/2012	SLN	Vitamin D3 and retinoic acid	Treatment of diseases like tuberculosis, age-related macular degeneration, diabetic retinopathy, cancers, hyperpigmentation, acne, and osteoporosis	[176]
Diagnostics delivery	WO2017041609	SLN	Gadopentetate dimeglumine	The MRI contrast agent gadopentetate dimeglumine is loaded into SLN that are freeze-dried with trehalose for easy intestinal uptake	[177]
	WO2014037498	SLN	Paramagnetic contrast agents	SLN are loaded with paramagnetic metals that are chelated by diazepine and tetraazocyclododecane compounds for in vivo applications	[178]
	WO2014191467	SLN	Cyanine dye and alkaline-earth metal	SLN are loaded with a fluorescent cyanine dye and alkaline-earth metals that are complexed by diazepine and tetraazocyclododecane compounds for in vivo applications	[179]
Miscellaneous	WO2014058179	SLN	—	LDL-like cationic SLN are suitable for liver-targeted delivery, for both the diagnosis and treatment of diseases	[180]
	CN200910192863	SLN	Emamectin	Emamectin benzoate-loaded SLN improve chemical stability in hot and cold storage, reducing the photolysis rate, prolonging efficacy time, reducing dosage, and significantly improving the insecticidal effect, as compared to raw emamectin benzoate pesticides	[181]