Nanostructured Lipid Carriers for Improved Delivery of Therapeutics via the Oral Route

Table 3

Site-specific delivery of medications via NLCs to the GIT.

Drug	Site of action	Model	Outcomes	References
Pumpkin seed oil	Stomach	In vivo pharmacokinetic studies	Pumpkin seed oil NLCs significantly reduced the ulcer index as compared to indomethacin and lessened mucosal lesions in comparison to pure pumpkin oil	[145]
Thymoquinone (THQ)	Stomach	In vivo efficacy studies against gastric ulcers	THQ suspension, blank coconut oil NLCs, and THQ-NLCs subdued the ulcerative index and hemorrhagic erosions on the gastric mucosa of mice due to ethanol-induced gastric ulcers	[146]
Sirolimus (SRL)	Intestine	In vitro lipolysis model/in vivo pharmacokinetic study	Nearly 100% drug loading, lipolysis caused fast digestion of NLCs, a 1.82-fold rise in oral bioavailability in comparison to conventional tablets in beagle dogs	[147]
Vincristine sulfate (VCR)	Intestine	Cellular uptake studies/in vivo pharmacokinetic study	Boosted two-fold oral bioavailability of VCR by prolonging the interaction between positively charged hyaluronic acid-modified NLCs (HA-NLCs) and negatively charged mucous membranes. The smaller size of NLCs enabled internalization into the gastric mucosa	[148]
Nabumetone (NBM)	Intestine	In vivo pharmacokinetic study	In vivo studies confirmed that NBM-NLCs can improve intestinal absorption of NEM when administered orally	[149]
Tacrolimus (TL)	Intestine	In vitro lipolysis study/in vivo pharmacokinetic/organ distribution studies	Higher drug solubility was observed than drug suspension alone. Bioavailability was significantly higher than the market formulation. Lymphatic uptake of NLC-N2 and NLC-C2 was significantly ( < 0.001) enhanced by 19.25- and 14.5- fold, at 1 h; 7.5- and 6.8-fold after 24 h, respectively, in comparison to TL suspension	[150]
Simvastatin and nifedipine	Intestine	In vivo pharmacodynamic studies	Simvastatin and nifedipine-loaded NLCs, both in combination significantly lowered the hypercholesteremic levels, and poloxamer 407 might also have improved the intestinal absorption of NLCs	[151]
Isradipine (ISD)	Intestine	In vitro gut permeation and in vivo solubilization	Cycloheximide (a lymphatic uptake inhibitor) absence increased the oral bioavailability of ISD by 4.2-fold, improved gut permeation, solubility, lymphatic uptake, and biodistribution	[152]
Budesonide (BSD)	Colon	In vitro (J774 murine macrophages)/in vivo colon localization study	BSD-NLCs and blank NLCs were retained for a longer duration in the mucosa, reduced TNF-α secretion, and coumarin-6-NLCs were localized for a prolonged time at the colon even after dextran sulfate- (DS-) induced colitis in mice	[153]
Celecoxib (CLX)	Colon	In vivo therapeutic efficacy study	Eudragit RS100-CLX-NLCs regained the disruption caused by DS-induced colitis in the mucosa, submucosa, and muscular layers of the colon of mice	[154]
Oleuropein (OPN)	Colon	In vivo efficacy studies against acute colitis	OPN suspension and OPN-NLCs regained the disruption caused in the structure of the colon by DS-induced colitis in mice	[155]