scholarly journals Orally Administrable Therapeutic Nanoparticles for the Treatment of Colorectal Cancer

2021 ◽  
Vol 9 ◽  
Author(s):  
Kangkang Ying ◽  
Bingjun Bai ◽  
Xing Gao ◽  
Yuzi Xu ◽  
Hangxiang Wang ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Drug Delivery ◽  
Water Solubility ◽  
Oral Drug Delivery ◽  
Local Drug Delivery ◽  
Oral Drug ◽  
Glycoprotein P ◽  
Therapeutic Outcomes ◽  
Poorly Soluble ◽  
Oral Therapeutic

Colorectal cancer (CRC) is one of the most common and lethal human malignancies worldwide; however, the therapeutic outcomes in the clinic still are unsatisfactory due to the lack of effective and safe therapeutic regimens. Orally administrable and CRC-targetable drug delivery is an attractive approach for CRC therapy as it improves the efficacy by local drug delivery and reduces systemic toxicity. Currently, chemotherapy remains the mainstay modality for CRC therapy; however, most of chemo drugs have low water solubility and are unstable in the gastrointestinal tract (GIT), poor intestinal permeability, and are susceptible to P-glycoprotein (P-gp) efflux, resulting in limited therapeutic outcomes. Orally administrable nanoformulations hold the great potential for improving the bioavailability of poorly permeable and poorly soluble therapeutics, but there are still limitations associated with these regimes. This review focuses on the barriers for oral drug delivery and various oral therapeutic nanoparticles for the management of CRC.

scholarly journals Self-Nano-Emulsifying Drug-Delivery Systems: From the Development to the Current Applications and Challenges in Oral Drug Delivery

Pharmaceutics ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 1194
Author(s):  
Aristote B. Buya ◽  
Ana Beloqui ◽  
Patrick B. Memvanga ◽  
Véronique Préat
Keyword(s):  
Drug Delivery ◽  
Patient Compliance ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Oral Drug Delivery ◽  
Delivery Systems ◽  
Oral Drug ◽  
Statistical Design Of Experiments

Approximately one third of newly discovered drug molecules show insufficient water solubility and therefore low oral bio-availability. Self-nano-emulsifying drug-delivery systems (SNEDDSs) are one of the emerging strategies developed to tackle the issues associated with their oral delivery. SNEDDSs are composed of an oil phase, surfactant, and cosurfactant or cosolvent. SNEDDSs characteristics, their ability to dissolve a drug, and in vivo considerations are determinant factors in the choice of SNEDDSs excipients. A SNEDDS formulation can be optimized through phase diagram approach or statistical design of experiments. The characterization of SNEDDSs includes multiple orthogonal methods required to fully control SNEDDS manufacture, stability, and biological fate. Encapsulating a drug in SNEDDSs can lead to increased solubilization, stability in the gastro-intestinal tract, and absorption, resulting in enhanced bio-availability. The transformation of liquid SNEDDSs into solid dosage forms has been shown to increase the stability and patient compliance. Supersaturated, mucus-permeating, and targeted SNEDDSs can be developed to increase efficacy and patient compliance. Self-emulsification approach has been successful in oral drug delivery. The present review gives an insight of SNEDDSs for the oral administration of both lipophilic and hydrophilic compounds from the experimental bench to marketed products.

Potential cardio-protective agents: A Resveratrol review (2000-2019).

2020 ◽  
Vol 26 ◽  
Author(s):  
Chahinez Houacine ◽  
Iftikhar Khan ◽  
Sakib Saleem Yousaf
Keyword(s):  
Drug Delivery ◽  
Clinical Effect ◽  
Water Solubility ◽  
Oral Drug Delivery ◽  
Oral Drug ◽  
Protective Agent ◽  
Physiochemical Properties ◽  
Area Of Interest ◽  
Therapeutic Compounds

: With a 2030 projection of 23.6 million deaths per year the prevalence and severity of cardiovascular disease is at an astounding high. Thus, a definitive need for the identification of novel compounds with potential to prevent or treat the disease and associated states. Moreover, there is also an ever-increasing need for drug delivery systems (DDS) that cope with poor and ranging physiochemical properties of therapeutic compounds to achieve clinical effect. The usage of resveratrol (RES) is a growing area of interest with innumerate pieces of research evidencing the drug’s efficacy. This drug is however marred, its notably poor physiochemical properties (namely poor water solubility) limits its use for oral drug delivery. RES analogues however, potentially possess superior physiochemical characteristics offering a remedy for the aforementioned drawback. However, particulate based DDS are equally able to offer property amelioration and targeting. This review offers an extensive examination into the role of RES as a potential cardio protective agent. The prevalence and suitability of associated analogues and the role of nanotechnology in overcoming physicochemical boundaries, particularly through the development of nanoparticulate formulations, will be discussed in detail.

Application of Drug Nanocrystal Technologies on Oral Drug Delivery of Poorly Soluble Drugs

2012 ◽  
Vol 30 (2) ◽  
pp. 307-324 ◽  
Author(s):  
Lei Gao ◽  
Guiyang Liu ◽  
Jianli Ma ◽  
Xiaoqing Wang ◽  
Liang Zhou ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Oral Drug ◽  
Poorly Soluble Drugs ◽  
Poorly Soluble ◽  
Drug Nanocrystal

scholarly journals Starch/Poly(glycerol-adipate) Nanocomposites: A Novel Oral Drug Delivery Device

Coatings ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 125
Author(s):  
Ambra Vestri ◽  
Amanda K. Pearce ◽  
Robert Cavanagh ◽  
Ioanna D. Styliari ◽  
Carlos Sanders ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Water Solubility ◽  
Oral Drug Delivery ◽  
Oral Drug ◽  
Biological Assays ◽  
Drug Delivery Device ◽  
Effective Activity ◽  
Vis Spectroscopy ◽  
Starch Films

Biocompatible and bio-based materials are an appealing resource for the pharmaceutical industry. Poly(glycerol-adipate) (PGA) is a biocompatible and biodegradable polymer that can be used to produce self-assembled nanoparticles (NPs) able to encapsulate active ingredients, with encouraging perspectives for drug delivery purposes. Starch is a versatile, inexpensive, and abundant polysaccharide that can be effectively applied as a bio-scaffold for other molecules in order to enrich it with new appealing properties. In this work, the combination of PGA NPs and starch films proved to be a suitable biopolymeric matrix carrier for the controlled release preparation of hydrophobic drugs. Dynamic Light Scattering (DLS) was used to determine the size of drug-loaded PGA NPs, while the improvement of the apparent drug water solubility was assessed by UV-vis spectroscopy. In vitro biological assays were performed against cancer cell lines and bacteria strains to confirm that drug-loaded PGA NPs maintained the effective activity of the therapeutic agents. Dye-conjugated PGA was then exploited to track the NP release profile during the starch/PGA nanocomposite film digestion, which was assessed using digestion models mimicking physiological conditions. The collected data provide a clear indication of the suitability of our biodegradable carrier system for oral drug delivery.

scholarly journals Pickering nano-emulsions stabilized by Eudragit RL100 nanoparticles as oral drug delivery system for poorly soluble drugs

2020 ◽  
Vol 191 ◽  
pp. 111010
Author(s):  
Sidy Mouhamed Dieng ◽  
Ziad Omran ◽  
Nicolas Anton ◽  
Oumar Thioune ◽  
Alphonse Rodrigue Djiboune ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Drug Delivery ◽  
Oral Drug ◽  
Poorly Soluble Drugs ◽  
Oral Drug Delivery System ◽  
Poorly Soluble

Oral Drug Delivery Systems for Ulcerative Colitis Therapy: A Comparative Study with Microparticles and Nanoparticles

2019 ◽  
Vol 19 (4) ◽  
pp. 304-311 ◽  
Author(s):  
Panpan Ma ◽  
Xiaoying Si ◽  
Qiubing Chen ◽  
Lijun Ma ◽  
Meili Hou ◽  
...  
Keyword(s):  
Ulcerative Colitis ◽  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Oral Drug ◽  
Average Particle ◽  
Oil Emulsion ◽  
In Vivo Experiments ◽  
Therapeutic Outcomes ◽  
Evaporation Technique

Background: Oral administrations of microparticles (MPs) and nanoparticles (NPs) have been widely employed as therapeutic approaches for the treatment of ulcerative colitis (UC). However, no previous study has comparatively investigated the therapeutic efficacies of MPs and NPs. Methods: In this study, curcumin (CUR)-loaded MPs (CUR-MPs) and CUR-loaded NPs (CUR-NPs) were prepared using a single water-in-oil emulsion solvent evaporation technique. Their therapeutic outcomes against UC were further comparatively studied. Results: The resultant spherical MPs and NPs exhibited slightly negative zeta-potential with average particle diameters of approximately 1.7 µm and 270 nm, respectively. It was found that NPs exhibited a much higher CUR release rate than MPs within the same period of investigation. In vivo experiments demonstrated that oral administration of CUR-MPs and CUR-NPs reduced the symptoms of inflammation in a UC mouse model induced by dextran sulfate sodium. Importantly, CUR-NPs showed much better therapeutic outcomes in alleviating UC compared with CUR-MPs. Conclusion: NPs can improve the anti-inflammatory activity of CUR by enhancing the drug release and cellular uptake efficiency, in comparison with MPs. Thus, they could be exploited as a promising oral drug delivery system for effective UC treatment.

Self-micro Emulsifying Drug Delivery System “SMEDDS” for Efficient Oral Delivery of Andrographolide

2020 ◽  
Vol 10 (1) ◽  
pp. 38-53 ◽  
Author(s):  
Sivaram Nallamolu ◽  
Vijaya R. Jayanti ◽  
Mallikarjun Chitneni ◽  
Liew Y. Khoon ◽  
Prashant Kesharwani
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Water Solubility ◽  
Oral Drug Delivery ◽  
Drug Loading ◽  
Oral Drug ◽  
Breast Cancer Cell Lines ◽  
Dissolution Profile

Objective: Andrographolide has potent anticancer and antimicrobial activity; however, its clinical application has been limited due to its poor water solubility as well as lack of appropriate formulation. The objective of this investigation was to formulate Self–Micro Emulsifying Drug Delivery System (SMEDDS) of andrographolide and explore its oral drug delivery aptitudes. Methods: Andrographolide SMEDDS was optimized by ternary phase approach and studied for various in vitro characteristics: Particle size, electron microscopy, polydispersity index, surface charge, dilution effect, pH stability, freeze-thaw effect, dissolution profile and stability studies. Further, antimicrobial and cytotoxic performance of andrographolide SMEDDS were evaluated in MCF–7 breast cancer cell lines and methicillin-resistant microorganisms, respectively. Results: An optimized SMEDDS formulation of andrographolide was successfully prepared and evaluated for its drug delivery potential. The solubility of andrographolide in the developed SMEDDS formulation was increased significantly, and the drug loading was enough for making this drug clinically applicable. The andrographolide SMEDDS formulation competitively inhibited the growth of microorganisms and showed enhanced anti–microbial activity against MRSA microorganisms. Conclusion: The SMEDDS strategy represents one of the best approaches to deliver andrographolide via oral route, while resolving its solubility limitations.

A Review on Recent Controlled Release Strategies for Oral Drug Delivery of Repaglinide (a BCS Class II Drug)

2021 ◽  
Vol 10 ◽  
Author(s):  
Saba Albetawi ◽  
Amer Abdalhafez ◽  
Ala Abu-Zaid
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Pancreatic Beta Cells ◽  
Water Solubility ◽  
Oral Drug Delivery ◽  
Aqueous Solubility ◽  
Class Ii ◽  
Oral Drug ◽  
Log P ◽  
P Value

: Repaglinide is an antidiabetic drug that works by stimulating insulin secretion from pancreatic beta cells. Repaglinide is practically insoluble in water with a water solubility of 34 µg/mL at 37 ˚C, and it has a high absorption rate from the gastrointestinal tract following oral administration since the log P value of repaglinide is 3.97. The low aqueous solubility and the high permeability of repaglinide represent a typical behavior for drugs that belong to class II Biopharmaceutical Classification System (BCS II). Managing type-2 diabetes mellitus with repaglinide is considered a burdensome therapy, as it requires frequent dosing of repaglinide before each meal to maintain its therapeutic plasma concentration due to its short plasma half-life of approximately one hour. Hence the present review aims to discuss thoroughly the various approaches investigated in recent years to develop drug delivery systems that improve oral delivery of repaglinide, including nanoemulsions, solid lipid nanoparticles, nanostructured lipid carriers, sustained-release hydrophilic matrix, floating microspheres, and nanocomposites.

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