7.2.2 Intercalated montmorillonite solid lipid nanoparticles

Betaxolol hydrochloride (BH) is widely used for the treatment of ocular hypertension and open-angle glaucoma in clinical therapeutics. However, it faces certain limitations like low bioavailability and pre-ocular retention, and some side effects.


Table 5.

List of SLNs and their different ligand conjugated forms for eye, colon and kidney targeting.

In order to overcome these limitations acid treated montmorillonite (Mt)- Betaxolol Hydrochloride (BH) nanocomposite encapsulated SLNs (Mt-BH-SLNs) were developed. An acid-treated montmorillonite (acid-Mt) was first intercalated with BH in the interlayers and this nanocomposite was encapsulated by SLNs. The developed Mt-BH-SLNs possess good stability. Long term irritation test reported that the (Mt-BH-SLNs) showed no damage for cornea and conjunctiva. The corneal hydration level of Mt-BH-SLNs was higher (78.25 0.63)% indicating higher drug corneal permeability and absence of irritation to the cornea. Thus, Mt-BH-SLNs could be used for effective management of glaucoma [70].

9. Solid lipid nanoparticles for kidney targeting

DOI: http://dx.doi.org/10.5772/intechopen.88268

Solid Lipid Based Nano-particulate Formulations in Drug Targeting

kidney diseases [76].

have been summarized in Table 5.

10. Conclusion

115

9.1 Solid lipid nanoparticles for passive kidney targeting

9.1.2 Sialic acid conjugated PEGylated solid lipid nanoparticles

E-selectin is a promising target for the site-specific delivery of anti-

inflammatory agents. Several researchers have reported that sialic acid (SA)-mediated micelles could be specifically internalized by lipopolysaccharide (LPS)-activated human umbilical vein endothelial cells (HUVECs) via the specific binding between SA and E-selectin receptor [77]. Sialic acid (SIA) conjugated PEGylated dexamethasone (DXM) loaded SLNs (SIA-PEGylated-DXM-SLN) were developed to deliver DXM specifically to the kidney and to improve the therapeutic efficacy of DXM for renal ischemia–reperfusion injury (IRI)-induced acute renal injury. The Sialic acid (SIA) conjugated PEGylated DXM (SIA-PEG-DXM) was synthesized by adding PEG-DXM, dicyclohexylcarbodiimide (DCC), and 4-dimethylaminopyridine (DMAP) into anhydrous dimethyl formamide (DMF) followed by addition of SIA into the solution. The resulting mixture was stirred for obtaining SIA-PEG-DXM. The crude product was purified by dialysis against deionized water for 2 days, followed by lyophilization. The developed SLNs potentially had good colloidal stability in human body. The study revealed that the apoptotic human umbilical vein endothelial cells (HUVECs) were significantly decreased. It indicated the suitability of SIA-PEGylated-SLNs for internalization by the inflamed vascular endothelial cells. Biodistribution study revealed higher renal accumulation of DXM (range 2.7- to 5.88-fold higher) after 6 h of intravenous administration. The Pharmacodynamic study revealed that higher blood biochemical indexes, histopathological changes, oxidative stress levels, and pro-inflammatory cytokines which indicated improved renal function by the influence of SIA-PEGylated DXM [64]. List of SLNs and their different ligand conjugated form targeting to the kidney

Though drug targeting to a specific site in the body is an interesting approach, it is a highly challenging task. Despite that a large variety of smart nanocarriers have been developed for drug targeting in recent years, SLN has achieved a special status among them and can be employed for both passive as well as active targeting. These can be

9.1.1 Polyethylene glycol (PEG) surface modified solid lipid nanoparticles

Icariin (IRN) is widely used as traditional Chinese medicine for the treatment of kidney diseases and reinforce yang. The PEG surface modified Icariin (IRN) loaded SLNs (PEG-IRN-SLNs) was developed for targeted delivery of IRN to the kidney and to improve the bioavailability. The SLN was prepared by high temperature melt-cool solidification method. Upon comparing with IRN solution it was revealed from the pharmacokinetic study that the biological half-life (t1/2) and area under curve (AUC) of PEG-IRN-SLN was 7-fold and 4-fold higher. Biodistribution study revealed that IRN concentration in kidney tissues was significantly increased. Moreover, the relative target efficiency to kidney tissues was 79% and relative tissue exposure was 16.95. Thus the develop SLN could be helpful in the treatment of
