Overview of nanoparticulate strategies for solubility enhancement of poorly soluble drugs

Khan, Kifayat Ullah; Minhas, Muhammad Usman; Badshah, Syed Faisal; Suhail, Muhammad; Ahmad, Aousaf; Ijaz, S.

doi:10.1016/j.lfs.2022.120301

Cited by 102 publications

(46 citation statements)

References 198 publications

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“…The internal cavity of the β-CD is highly lipophilic, while the external surface is hydrophilic. Whenever any drug is loaded in a β-CD-based drug delivery system, the hydrophobic abilities of the drug are mostly restrained by the internal lipophilic cavity of the polymer, whereas the hydrophilic abilities remain exposed to the external environment; hence, the hydrophilicity of the drug is enhanced and the maximum drug concentration is solubilized in the respective media [ 55 ]. Furthermore, the hydroxyl and amino groups of carboxy methyl chitosan result in significant protonation in neutral solution and increase carboxy methyl chitosan’s solubility in neutral and basic solutions without influencing other important characteristics.…”

Section: Resultsmentioning

confidence: 99%

Synthesis and Characterization of Carboxymethyl Chitosan Nanosponges with Cyclodextrin Blends for Drug Solubility Improvement

Rizvi

Akhtar

Minhas

et al. 2022

Gels

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This study aimed to enhance the solubility and release characteristics of docetaxel by synthesizing highly porous and stimuli responsive nanosponges, a nano-version of hydrogels with the additional qualities of both hydrogels and nano-systems. Nanosponges were prepared by the free radical polymerization technique and characterized by their solubilization efficiency, swelling studies, sol-gel studies, percentage entrapment efficiency, drug loading, FTIR, PXRD, TGA, DSC, SEM, zeta sizer and in vitro dissolution studies. In vivo toxicity study was conducted to assess the safety of the oral administration of prepared nanosponges. FTIR, TGA and DSC studies confirmed the successful grafting of components into the stable nano-polymeric network. A porous and sponge-like structure was visualized through SEM images. The particle size of the optimized formulation was observed in the range of 195 ± 3 nm. The fabricated nanosponges noticeably enhanced the drug loading and solubilization efficiency of docetaxel in aqueous media. The drug release of fabricated nanosponges was significantly higher at pH 6.8 as compared to pH 1.2 and 4.5. An acute oral toxicity study endorsed the safety of the system. Due to an efficient preparation technique, as well as its enhanced solubility, excellent physicochemical properties, improved dissolution and non-toxic nature, nanosponges could be an efficient and a promising approach for the oral delivery of poorly soluble drugs.

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Section: Resultsmentioning

confidence: 99%

Synthesis and Characterization of Carboxymethyl Chitosan Nanosponges with Cyclodextrin Blends for Drug Solubility Improvement

Rizvi

Akhtar

Minhas

et al. 2022

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“…Solubility was improved due to the hydrophilic and highly amorphous nature of the prepared nanomatrices. Kifayat et al also reported the solubility enhancement of the poorly soluble drug olanzapine by developing nanomatrices using a different composition of hydrophilic ingredients [ 29 ]. Polymer chitosan has already been used previously for solubility enhancement of carvedilol, nifedipine, and curcumin [ 3 , 51 , 52 ].…”

Section: Resultsmentioning

confidence: 99%

“…Nanomatrices are a highly responsive polymeric network that abruptly swell upon contact with aqueous medium due to their highly amorphous nature and porous structure, and the entrapped drug immediately releases into the surrounding media [ 29 ]. The release mechanism from cross-linked nanomatrices is shown in Figure 7 c.…”

Section: Resultsmentioning

confidence: 99%

“…Based upon the size of the obtained particles, hydrogels can be classified as macrogels, microgels, and nanogels/nanomatrices. Hydrogel particles fabricated in the nanometer range are termed as nanogels/nanomatrices [ 29 ], particles obtained in the micrometer range are termed as microgels, and particles bigger than micrometer range are termed as macrogels [ 30 ].…”

Section: Introductionmentioning

confidence: 99%

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Highly Responsive Chitosan-Co-Poly (MAA) Nanomatrices through Cross-Linking Polymerization for Solubility Improvement

Saleem

Akhtar

Minhas

et al. 2022

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In this study, we report the highly responsive chitosan-based chemically cross-linked nanomatrices, a nano-version of hydrogels developed through modified polymerization reaction for solubility improvement of poorly soluble drug simvastatin. The developed nanomatrices were characterized for solubilization efficiency, swelling studies, sol-gel analysis, in vitro drug release studies, DSC, FTIR, XRD, SEM, particle size analysis, and stability studies. An in vivo acute toxicity study was conducted on female Winstor rats, the result of which endorsed the safety and biocompatibility of the system. A porous and fluffy structure was observed under SEM analysis, which supports the great swelling tendency of the system that further governs the in vitro drug release. Zeta sizer analyzed the particle size in the range of 227.8 ± 17.8 nm. Nano sizing and grafting of hydrophilic excipients to the nanomatrices system explains this shift of trend towards the enhancement of solubilization efficiency, and, furthermore, the XRD results confirmed the amorphous nature of the system. FTIR and DSC analysis confirmed the successful grafting and stability to the system. The developed nanomatrices enhanced the release characteristics and solubility of simvastatin significantly and could be an effective technique for solubility and bioavailability enhancement of other BCS class-II drugs. Due to enhanced solubility, efficient method of preparation, excellent physico-chemical features, and rapid and high dissolution and bio-compatibility, the developed nanomatrices may be a promising approach for oral delivery of hydrophobic drugs.

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“…On account of inadequately water-solvent medications, disintegration is the rate-constraining advance during the time spent medication retention. At the point when a functioning specialist is managed orally, it should initially break down in gastric as well as intestinal liquids before it can pervade the films of the GIT to arrive at foundational dissemination and thus two territories of pharmaceutical research that attention on improving the oral bioavailability of dynamic operators incorporate; upgrading of dissolvability and disintegration pace of ineffectively water solvent drugs [1][2][3]. It is notable that low watery solvency of the new pharmaceutical dynamic operator is an issue for the pharmaceutical advancement process which ought to be tended to at an opportune time during compound improvement [4][5][6].…”

Section: Introductionmentioning

confidence: 99%

Triazine Dendrimers: An Excellent Drug Carrier for Improving the Solubility of Glyburide an Antidiabetic Agent

Malek¹,

Patel²

2022

Preprint

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The intent of this work was to synthesized, develop and characterize a novel dendrimer and drug-dendrimer solutions to resolve poorly aqueous solubility of glyburide which is an antidiabetic BSC class-II drug’s problem. Drug- dendrimer complex formation is one of the widely reported method for solubility enhancement of the drug which can increase the efficiency of the drug. A number of glyburide drug solutions were formulated with different quantities of G1, G2 and G3 dendrimers via Higuchi and Connors method. The effects of pH, dendrimer concentration and generation of dendrimers (G1-G3) on the aqueous solubility of drug was investigated and characterized by FT-IR, NMR ( 1 H and 13 C). The experimental outcomes recommended that solubility of glyburide was significantly enhanced with the increasing concentration of dendrimers as well as the generations of dendrimers.

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Overview of nanoparticulate strategies for solubility enhancement of poorly soluble drugs

Cited by 102 publications

References 198 publications

Synthesis and Characterization of Carboxymethyl Chitosan Nanosponges with Cyclodextrin Blends for Drug Solubility Improvement

Synthesis and Characterization of Carboxymethyl Chitosan Nanosponges with Cyclodextrin Blends for Drug Solubility Improvement

Highly Responsive Chitosan-Co-Poly (MAA) Nanomatrices through Cross-Linking Polymerization for Solubility Improvement

Triazine Dendrimers: An Excellent Drug Carrier for Improving the Solubility of Glyburide an Antidiabetic Agent

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