Investigation of drug-polymer miscibility, biorelevant dissolution, and bioavailability improvement of Dolutegravir-polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer solid dispersions

Lakshman, Dani; Chegireddy, Mohith; Hanegave, Geeta K.; Sree, K. Navya; Kumar, N.S. Krishna; Lewis, Shaila; Dengale, Swapnil J.

doi:10.1016/j.ejps.2019.105137

Cited by 38 publications

(31 citation statements)

References 45 publications

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“…Further, if the polymer possesses surfactant properties, then partitioning of the drug in the micelles may help in improving the solubility. Such solubility advantage may be over, and above the solubility, the advantage gained through high energy amorphous state (55)(56)(57). The hydrophilic and amorphous polymers are deliquescent in nature.…”

Section: Selection Criteria For Polymeric Carriersmentioning

confidence: 99%

“…Lakshman et al ., (2020) found that the dissolution advantage of API from Dolutegravir/Soluplus® dispersion in USP phosphate buffer pH 6.8 was found bridged in biorelevant media. The bridging in the dissolution extent was due to the improvement of dissolution of pure Dolutegravir in biorelevant media which is attributed to micellar solubilization of Dolutegravir in the bile and lecithin micelles, and much less due to the retardation of dissolution from solid dispersion ( 56 ).…”

Section: Soluplus®mentioning

confidence: 99%

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Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

et al. 2020

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Solid dispersion is the preferred technology to prepare efficacious forms of BCS class-II/IV APIs. To prepare solid dispersions, there exist a wide variety of polymeric carriers with interesting physicochemical and thermochemical characteristics available at the disposal of a formulation scientist. Since the advent of the solid dispersion technology in the early 1960s, there have been more than 5000 scientific papers published in the subject area. This review discusses the polymeric carrier properties of most extensively used polymers PVP, Copovidone, PEG, HPMC, HPMCAS, and Soluplus® in the solid dispersion technology. The literature trends about preparation techniques, dissolution, and stability improvement are analyzed from the Scopus® database to enable a formulator to make an informed choice of polymeric carrier. The stability and extent of dissolution improvement are largely dependent upon the type of polymeric carrier employed to formulate solid dispersions. With the increasing acceptance of transfer dissolution setup in the research community, it is required to evaluate the crystallization/precipitation inhibition potential of polymers under dynamic pH shift conditions. Further, there is a need to develop a regulatory framework which provides definition and complete classification along with necessarily recommended studies to characterize and evaluate solid dispersions.

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Section: Selection Criteria For Polymeric Carriersmentioning

confidence: 99%

Section: Soluplus®mentioning

confidence: 99%

Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

et al. 2020

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“…Elements with likely values of

are considered miscible. A difference of

value less than 7 (MPa) 0.5 predicts adequate [ 58 ]. The Flory-Huggins interaction parameter, derived from the melting point depression method, can also be used in molecular interaction studies between two components [ 59 ].…”

Section: Amorphous Drug Loaded Transdermal Systemsmentioning

confidence: 99%

Amorphization of Drugs for Transdermal Delivery-a Recent Update

et al. 2022

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Amorphous solid dispersion is a popular formulation approach for orally administered poorly water-soluble drugs, especially for BCS class II. But oral delivery could not be an automatic choice for some drugs with high first-pass metabolism susceptibility. In such cases, transdermal delivery is considered an alternative if the drug is potent and the dose is less than 10 mg. Amorphization of drugs causes supersaturation and enhances the thermodynamic activity of the drugs. Hence, drug transport through the skin could be improved. The stabilization of amorphous system is a persistent challenge that restricts its application. A polymeric system, where amorphous drug is dispersed in a polymeric carrier, helps its stability. However, high excipient load often becomes problematic for the polymeric amorphous system. Coamorphous formulation is another approach, where one drug is mixed with another drug or low molecular weight compound, which stabilizes each other, restricts crystallization, and maintains a single-phase homogenous amorphous system. Prevention of recrystallization along with enhanced skin permeation has been observed by the transdermal coamorphous system. But scalable manufacturing methods, extensive stability study and in-depth in vivo evaluation are lacking. This review has critically studied the mechanistic aspects of amorphization and transdermal permeation by analyzing recent researches in this field to propose a future direction.

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“…It is also proposed to increase the solubility and bioavailability of poorly soluble molecules through the formed micelles. Moreover, as a polymer, it has a tendency not to absorb moisture from the air [ 116 , 117 ].…”

Section: Excipients Used In Ocular Formulations For Modified Drug Deliverymentioning

confidence: 99%

Recent Advances in the Excipients Used for Modified Ocular Drug Delivery

et al. 2021

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In ocular drug delivery, maintaining an efficient concentration of the drug in the target area for a sufficient period of time is a challenging task. There is a pressing need for the development of effective strategies for drug delivery to the eye using recent advances in material sciences and novel approaches to drug delivery. This review summarizes the important aspects of ocular drug delivery and the factors affecting drug absorption in the eye including encapsulating excipients (chitosan, hyaluronic acid, poloxamer, PLGA, PVCL-PVA-PEG, cetalkonium chloride, and gelatin) for modified drug delivery.

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Investigation of drug-polymer miscibility, biorelevant dissolution, and bioavailability improvement of Dolutegravir-polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer solid dispersions

Cited by 38 publications

References 45 publications

Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

Amorphization of Drugs for Transdermal Delivery-a Recent Update

Recent Advances in the Excipients Used for Modified Ocular Drug Delivery

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