Lipid Nanoparticles for the Delivery of Active Natural Medicines

Xing, Huijie; Wang, Huan; Wu, Baojian; Zhang, Qizhou

doi:10.2174/1381612824666171128105853

Cited by 13 publications

(8 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…More than 100 years ago, Paul Ehrlich envisioned an ideal drug carrier with following characteristics: long circulation duration/time, targeting ability, drug loading and drug release capacity, and bio-compatibility and non-toxicity [6] . Based on this assumption, with the continuous development of science and technology, various types of drug carriers have been prepared, such as nanomaterials [7] , [8] , [9] , [10] , [11] , [12] , [13] , [14] , [15] , [16] , controlled-release microspheres [17] , [18] , [19] , [20] , [21] , [22] , natural cell membranes [23] , [24] , [25] , [26] , [27] , [28] , [29] , [30] , [31] etc. These drug carriers can deliver not only small molecule drugs but also biological macromolecules, such as peptides and proteins.…”

Section: Introductionmentioning

confidence: 99%

Size, shape, charge and “stealthy” surface: Carrier properties affect the drug circulation time in vivo

Di¹,

Gao²,

Du³

et al. 2021

Asian Journal of Pharmaceutical Sciences

143

104

View full text Add to dashboard Cite

The present review sets out to discuss recent developments of the effects and mechanisms of carrier properties on their circulation time. For most drugs, sufficient in vivo circulation time is the basis of high bioavailability. Drug carrier plays an irreplaceable role in helping drug avoid being quickly recognized and cleared by mononuclear phagocyte system, to give drug enough time to arrive at targeted organ and tissue to play its therapeutic effect. The physical and chemical properties of drug carriers, such as size, shape, surface charge and surface modification, would affect their in vivo circulation time, metabolic behavior and biodistribution. The final circulation time of carriers is determined by the balance between macrophage recognitions, blood vessel penetration and urine excretion. Therefore, when designing the drug delivery system, we should pay much attention to the properties of drug carriers to get enough in vivo circulation time to arrive at target site eventually. This article mainly reviews the effect of carrier size, size, surface charge and surface properties on its circulation time in vivo , and discusses the mechanism of these properties affecting circulation time. This review has reference significance for the research of long-circulation drug delivery system.

show abstract

Section: Introductionmentioning

confidence: 99%

Size, shape, charge and “stealthy” surface: Carrier properties affect the drug circulation time in vivo

Di¹,

Gao²,

Du³

et al. 2021

Asian Journal of Pharmaceutical Sciences

143

104

View full text Add to dashboard Cite

show abstract

“…These three materials were adopted on purpose to construct bioadhesive nanocarrier based on their respective functions. ATO 5 is a solid lipid above the body temperature that can guarantee high drug entrapment and sustained drug release (Xing et al, 2018). Carbomers with a brand name Carbopol, are synthetic macromolecular polymers based on acrylic acid that are crosslinked with either allyl sucrose or allyl ethers of pentaerythritol.…”

Section: Preparation and Characterization Of Rlx-bnpsmentioning

confidence: 99%

Bioadhesive polymer/lipid hybrid nanoparticles as oral delivery system of raloxifene with enhancive intestinal retention and bioavailability

Gao²,

Song

2021

Drug Delivery

View full text Add to dashboard Cite

Raloxifene (RLX) is a second-generation selective estrogen receptor modulator used to treat osteoporosis in postmenopausal women. RLX fails to be developed into injectable dosage forms due to poor solubility. Although oral formulations are clinically available, the lower bioavailability (<2%) embarrasses the pharmaceutists. This work reported a bioadhesive nanosystem intended for oral delivery of RLX to enhance its oral bioavailability and address the formulation challenge. The bioadhesive nanosystem refers to polymer-lipid hybrid nanoparticles made up of Carbopol 940, glyceryl distearate, and TGPS. RLX was solidly encapsulated into bioadhesive nanoparticles (bNPs) through a nanoprecipitation technique along with synchronous desalting of RLXÁHCl. The resultant RLX-loaded bNPs (RLX-bNPs) were characterized by particle size, f potential, morphology, and entrapment efficiency. The in vitro release and in vivo oral bioavailability of RLX-bNPs in rats were comparatively investigated with RLXloaded common lipid nanoparticles (RLX-cNPs). The preferred formulation possesses a particle size of 150 nm around with a polydispersity index (PDI) of 0.282. RLX-bNPs exhibited slower drug release than RLX-cNPs owing to the presence of an adhesive layer. After oral administration, RLX-bNPs resulted in significant enhancement in the bioavailability of RLX, up to 556.9% relative to RLX suspensions, while it was merely 244.7% for RLX-cNPs. Cellular testing and ex vivo transport imaging demonstrated that bNPs were endowed with excellent intestinal epithelial affinity and absorbability. Our study affords an alternative option for designing a suitable oral delivery system specific to amphiphobic drugs like RLXÁHCl.

show abstract

“…Solid lipid nanoparticles (SLNs) represent the first generation of lipid nanoparticles composed of a high-melting-point solid lipid and a small number of surfactant, which are developed on the base of from O/W emulsions [ 20 ]. SLNs present a solid state both at room and body temperature, thus possessing high physical stability.…”

Section: Lipid Dispersion Techniquementioning

confidence: 99%

“…Although lipid carriers have been proven to be potential as oral delivery vehicles, it should be noted that the lipolysis of lipid carriers substantially takes place in the gastrointestinal transport process. As a matter of fact, the in vivo degradation of lipid nanoparticles is not contradictory with their absorption-promoting effect, since lipids can facilitate drug absorption by co-transport and cytosis in the form of intact nanoparticles or reconstituted micelles [ 20 ]. The in vivo lipolysis-reconstitution mechanism of lipid nanocarriers have been confirmed by Wu’s laboratory utilizing an environment-responsive probe [ 179 , 180 ].…”

Section: Lipid Dispersion Techniquementioning

confidence: 99%

“…In addition to providing a supersaturated drug concentration in the gastrointestinal tract, lipid formulations have the advantages of motivating intestinal lymphatic drug transport and optimizing enterocyte-based drug transport and disposition whereby to reduce the first-pass effect and increase the lipophilic drug’s absorption [ 18 ]. The potential utility of lipid formulations as a means of bioavailability enhancer for poorly water-soluble drugs has been critically reviewed [ 19 , 20 ].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

et al. 2018

Self Cite

View full text Add to dashboard Cite

Over the past decades, a large number of drugs as well as drug candidates with poor dissolution characteristics have been witnessed, which invokes great interest in enabling formulation of these active ingredients. Poorly water-soluble drugs, especially biopharmaceutical classification system (BCS) II ones, are preferably designed as oral dosage forms if the dissolution limit can be broken through. Minimizing a drug’s size is an effective means to increase its dissolution and hence the bioavailability, which can be achieved by specialized dispersion techniques. This article reviews the most commonly used dispersion techniques for pharmaceutical processing that can practically enhance the dissolution and bioavailability of poorly water-soluble drugs. Major interests focus on solid dispersion, lipid-based dispersion (nanoencapsulation), and liquisolid dispersion (drug solubilized in a non-volatile solvent and dispersed in suitable solid excipients for tableting or capsulizing), covering the formulation development, preparative technique and potential applications for oral drug delivery. Otherwise, some other techniques that can increase the dispersibility of a drug such as co-precipitation, concomitant crystallization and inclusion complexation are also discussed. Various dispersion techniques provide a productive platform for addressing the formulation challenge of poorly water-soluble drugs. Solid dispersion and liquisolid dispersion are most likely to be successful in developing oral dosage forms. Lipid-based dispersion represents a promising approach to surmounting the bioavailability of low-permeable drugs, though the technique needs to traverse the obstacle from liquid to solid transformation. Novel dispersion techniques are highly encouraged to develop for formulation of poorly water-soluble drugs.

show abstract

Lipid Nanoparticles for the Delivery of Active Natural Medicines

Abstract: The survey shows that lipid nanoparticles are promising vehicles for the delivery of various natural actives and may address some intractable problems associated with delivery thereof.

Cited by 13 publications

References 0 publications

Size, shape, charge and “stealthy” surface: Carrier properties affect the drug circulation time in vivo

Size, shape, charge and “stealthy” surface: Carrier properties affect the drug circulation time in vivo

Bioadhesive polymer/lipid hybrid nanoparticles as oral delivery system of raloxifene with enhancive intestinal retention and bioavailability

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

Contact Info

Product

Resources

About