Lipid polymer hybrid as emerging tool in nanocarriers for oral drug delivery

Figures & data

Table I. List of permeation enhancers.

S. No.	Permeation enhancers
1	23-lauryl ether
2	Aprotinin
3	Benzalkonium chloride
4	Cyclodextrin
5	Dextran sulfate
6	Laurie acid/Propylene glycol
7	Oleic acid
8	Phosphatidylcholine
9	Sodium glycocholate
10	Menthol
11	Sodium N-[8-(2-hydroxy benzoyl) amino]caprylate (SNAC)
12	Sodium caprate

Figure 1. Difference between targeted and untargeted drug delivery system.

Table II. Types of lipid based formulations.

S. No.	Types	Examples
1.	Liquid lipid-based formulations	Emulsions or micro-emulsions, self-emulsifying drug delivery systems, self-nanoemulsified drug delivery systems, solid in oil suspension
2.	Solid lipid-based formulations	Solid state micro-emulsions, solid self-emulsifying drug delivery system for dry emulsions, microspheres, nanoparticles, suppositories
3.	Lipid as colloidal carriers	Liposomes, solid lipid nanoparticles (SLNs)

Table III. Types of excipients used in lipid based formulations.

S. No.	Excipients	Advantages	Example
1.	Triglycerides - Long chain triglycerides (TGs) - Medium chain TGs - Short chain TGs	Fully absorbed and consumed by body (Shegokar et al. 2011), medium chain TGs are less susceptible to oxidation (Gabizon 2001)	Caprylic acid, lauric acid, palmitic acid, oleic acid, behenic acid
2.	Mixed glycerides and polar oils	Promote emulsification (Montasser et al. 2013, Wong et al. 2007)	Sorbiton Trioleate (span 85), oleic acid
3.	Co-solvents	To promote solubilization (Montasser et al. 2013, Wong et al. 2007)	Ethanol, glycerol, propylene glycol and polyethylene glycol
4.	Water-insoluble surfactants	HLB of 8–12 can adsorb at oil-water interface	Polyoxyethylene, sorbitan trioleate (Tween-85), polyoxyethylene (Wong et al. 2007)
5.	Water-soluble surfactants	HLB of 12 or more	Alkyl ether ethoxylate, cremophor RH40 and RH60 (ethoxylated hydrogenated castor oil)
6.	Anti-oxidants	Protection from oxidation	α-tocopherol, β-carotene, propyl gallate, butylatedhydroxyltoluene (BHT)

Figure 2. Development of lipid polymer hybrid NPs.

Figure 3. Schematic representation of polymer core-lipid shell NPs.

Figure 4. Schematic representation of Hollow core/shell lipid– polymer–lipid hybrid NPs.

Figure 5. Schematic representation of mixed lipid polymer NPs.

Figure 6. Types of polymersomes.

Figure 7. Schematic representation of polymer caged NPs.

Figure 8. Scheme for uptake of nanoparticulate system through oral route.

Figure 9. Types of method of preparation for LPNs.

Figure 10. Schematic representation of double emulsification method.

Table 4. Studies performed to explore the potential of Lipid polymer hybrid nanoparticles in drug delivery.

S. No.	Drug	Size (nm)	Inference	Reference
1.	Vincristine sulfate	133.0 ± 8.2	High encapsulation efficiency, sustained release characteristics, acceptable biocompatibility, high drug encapsulation efficiency for cationic water soluble drugs and P-gp inhibition effect.	(Ling et al., 2010)
2.	FITC-labeled gelatin nanoparticles	100	Nanoparticle-in-microsphere oral delivery system of size less than 10 μm can be used for oral mucosal delivery of proteins, peptides and small drug molecules and larger size particles can be used for controlled release of drugs in the gastrointestinal tract.	(Bhavsar et al., 2006)
3.	Zidovudine	175 ± 2.5	Strong hydrogen bonding and hydrophobic interactions in polymer, lipid and therapeutic moiety, an elastic nature of the LPN, better entrapment of hydrophillic drugs and optimized drug release.	(Kumbhar and Pokharkar, 2013)
4.	Vinculin	106	LPNs possess stealth effect and prevent the negative effect of serum to intracellular compartment of cells, able to accumulate in cytoplasm.	(Wang et al., 2012a)
5.	Levofloxacin	420 ± 30	Spray freeze drying is better than spray drying in size, yield, flowability and aerosolization efficiency.	(Wang et al., 2012b)
6.	Doxorubicin	290	Enhanced drug uptake and retention time, improved nuclear localization and membrane associated P-gp can be bypassed and decreases drug resistance.	(Wong et al., 2006a)
7.	Small Interfering RNA delivery	225 ± 8	Gene silencing, higher efficiency, enhanced intracellular uptake via receptor mediated endocytosis.	(Shi et al., 2011)
8.	Anti-Carcino embryonic antigen half antibody	83–95	LPNs are responsible for specific targeting in pancreatic cancer.	(Hu et al., 2010)
9.	Paclitaxel	200–300	Inhibition of tumor growth, reduced toxicity, carboxymethyl chitosan provides gastric resistance, mucoadhesiveness to hybrid nanovesicles.	(Joshi et al., 2013)
10.	HEK293 and MDA-MB-231 cells	128	Useful in development of novel non-viral gene transfer vectors.	(Li et al., 2010)

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