Cellulose based polymers in development of amorphous solid dispersions

Chavan, Rahul B.; Rathi, Sneha; Jyothi, Vaskuri G.S. Sainaga; Shastri, Nalini R.

doi:10.1016/j.ajps.2018.09.003

Cited by 99 publications

(63 citation statements)

References 77 publications

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“…Though hydrophilic polymeric carriers appear an ideal choice for solid dispersion, being hydrophilic, they exhibit very limited solubility with usually hydrophobic drugs (BCS-II & IV). So, to molecularly dissolve a drug, large quantities of polymers are required (12,41,42). Further, hydrophilic polymers are deliquescent.…”

Section: Classification Of Polymeric Carriersmentioning

confidence: 99%

“…Further, hydrophilic polymers are deliquescent. The limited drug loading in a high proportion of polymer and deliquescent nature of hydrophilic polymers compounds the problem of phase separation, rendering the solid dispersion physically unstable (16,41,43,44). However, hydrophilic polymeric carriers have been demonstrated to be very efficient in solubility and dissolution improvement.…”

Section: Classification Of Polymeric Carriersmentioning

confidence: 99%

“…Owing to the availability of multiple cellulosic polymers and extensive scientific records thereof, the discussion under this section will be restricted to the prominently used cellulosic polymer in solid dispersion technology, i.e., HPMC & HPMCAS. The interested readers are advised to follow the rigorous review of the cellulosic polymers (41).…”

Section: Poly Ethylene Glycol (Peg)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: Classification Of Polymeric Carriersmentioning

confidence: 99%

Section: Classification Of Polymeric Carriersmentioning

confidence: 99%

Section: Poly Ethylene Glycol (Peg)mentioning

confidence: 99%

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Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

et al. 2020

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“…Several studies have identified hydroxypropylmethylcellulose acetate succinate (HPMCAS), which is a rather hydrophobic polymer, as a well-suited precipitation inhibitor for supersaturated solutions of CXB [18,20,21]. In general, HPMCAS is a polymer which was, in many cases, successfully applied for the formulation of amorphous solid dispersions [22][23][24][25]. However, there is no report about a binary ASD consisting of CXB and HPMCAS, which reached as high a concentration as theoretically expectable based on the precipitation inhibitory potential.…”

Section: Introductionmentioning

confidence: 99%

Impact of HPMCAS on the Dissolution Performance of Polyvinyl Alcohol Celecoxib Amorphous Solid Dispersions

Monschke

Wagner

2020

Pharmaceutics

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Amorphous solid dispersions (ASDs) have been proven to increase the bioavailability of poorly soluble drugs. It is desirable that the ASD provide a rapid dissolution rate and a sufficient stabilization of the generated supersaturation. In many cases, one polymer alone is not able to provide both features, which raises a need for reasonable polymer combinations. In this study we aimed to generate a rapidly dissolving ASD using the hydrophilic polymer polyvinyl alcohol (PVA) combined with a suitable precipitation inhibitor. Initially, PVA and hydroxypropylmethylcellulose acetate succinate (HPMCAS) were screened for their precipitation inhibitory potential for celecoxib in solution. The generated supersaturation in presence of PVA or HPMCAS was further characterized using dynamic light scattering. Binary ASDs of either PVA or HPMCAS (at 10% and 20% drug load) were prepared by hot-melt extrusion and solid-state analytics were conducted using differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD) and fourier-transformed infrared spectroscopy (FT-IR). The non-sink dissolution studies of the binary ASDs revealed a high dissolution rate for the PVA ASDs with subsequent precipitation and for the HPMCAS ASDs a suppressed dissolution. In order to utilize the unexploited potential of the binary ASDs, the PVA ASDs were combined with HPMCAS either predissolved or added as powder and also formulated as ternary ASD. We successfully generated a solid formulation consisting of the powdered PVA ASD and HPMCAS powder, which was superior in monophasic non-sink dissolution and biorelevant biphasic dissolution studies compared to the binary and ternary ASDs.

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“…Recent studies have shown that hydrophilic polymers, such as hydroxypropyl methylcellulose, polyvinylpyrrolidone, hydroxypropyl cellulose, and polyethylene glycol, are commonly used in the formation of SDs [18][19][20][21][22][23][24][25][26][27][28][29][30]. Moreover, ternary SDs of these polymers have also been utilized to further improve drug bioavailability [31][32][33][34][35][36][37][38][39][40][41].…”

Section: Introductionmentioning

confidence: 99%

Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

Tran

2020

Polymers

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In recent decades, solid dispersions have been demonstrated as an effective approach for improving the bioavailability of poorly water-soluble drugs, as have solid dispersion techniques that include the application of nanotechnology. Many studies have reported on the ability to change drug crystallinity and molecular interactions to enhance the dissolution rate of solid dispersions using hydrophilic carriers. However, numerous studies have indicated that insoluble carriers are also promising excipients in solid dispersions. In this report, an overview of solid dispersion strategies involving insoluble carriers has been provided. In addition to the role of solubility and dissolution enhancement, the perspectives of the use of these polymers in controlled release solid dispersions have been classified and discussed. Moreover, the compatibility between methods and carriers and between drug and carrier is mentioned. In general, this report on solid dispersions using insoluble carriers could provide a specific approach and/or a selection of these polymers for further formulation development and clinical applications.

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Cellulose based polymers in development of amorphous solid dispersions

Cited by 99 publications

References 77 publications

Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

Impact of HPMCAS on the Dissolution Performance of Polyvinyl Alcohol Celecoxib Amorphous Solid Dispersions

Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

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