pH-responsive dual pulse multiparticulate dosage form for treatment of rheumatoid arthritis

Lotlikar, Vishwanath; Kedar, Uttam; Shidhaye, Supriya; Kadam, Vilasrao

doi:10.3109/03639041003786185

Cited by 16 publications

(8 citation statements)

References 17 publications

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“…Pure Eudragit® S100, Eudragit® L100-55 and F3 physical mixture exhibited a broad endotherm at the temperature range between 50 and 100°C, attributed to water evaporation. Eudragit® S100 and Eudragit® L100-55 showed an endothermic peak at 218 and 203°C, respectively (37,38). For F3 Eudragit®-based filament, a broad decomposition endotherm was observed at 217°C.…”

Section: Differential Scanning Calorimetrymentioning

confidence: 99%

Controlled Release of 5-Fluorouracil from Alginate Beads Encapsulated in 3D Printed pH-Responsive Solid Dosage Forms

et al. 2018

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Three-dimensional printing is being steadily deployed as manufacturing technology for the development of personalized pharmaceutical dosage forms. In the present study, we developed a hollow pH-responsive 3D printed tablet encapsulating drug loaded non-coated and chitosan-coated alginate beads for the targeted colonic delivery of 5-fluorouracil (5-FU). A mixture of Eudragit® L100-55 and Eudragit® S100 was fabricated by means of hot-melt extrusion (HME) and the produced filaments were printed utilizing a fused deposition modeling (FDM) 3D printer to form the pH-responsive layer of the tablet with the rest comprising of a water-insoluble poly-lactic acid (PLA) layer. The filaments and alginate particles were characterized for their physicochemical properties (thermogravimetric analysis, differential scanning calorimetry, X-ray diffraction), their surface topography was visualized by scanning electron microscopy and the filaments' mechanical properties were assessed by instrumented indentation testing and tensile testing. The optimized filament formulation was 3D printed and the structural integrity of the hollow tablet in increasing pH media (pH 1.2 to pH 7.4) was assessed by means of time-lapsed microfocus computed tomography (μCT). In vitro release studies demonstrated controlled release of 5-FU from the alginate beads encapsulated within the hollow pH-sensitive tablet matrix at pH values corresponding to the colonic environment (pH 7.4). The present study highlights the potential of additive manufacturing in fabricating controlled-release dosage forms rendering them pertinent formulations for further in vivo evaluation.

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Section: Differential Scanning Calorimetrymentioning

confidence: 99%

Controlled Release of 5-Fluorouracil from Alginate Beads Encapsulated in 3D Printed pH-Responsive Solid Dosage Forms

et al. 2018

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“…Interestingly, a pH-responsive dual pulse multiparticulate dosage compund containing ketoprofen, was tested in RA and was found able to control circadian symptoms during midnight and early morning [ 52 ].…”

Section: Other Approaches To Chronotherapy In Rheumatoid Arthritismentioning

confidence: 99%

Glucocorticoid management in rheumatoid arthritis: morning or night low dose?

Paolino¹,

Cutolo²,

Pizzorni³

2017

Reumatologia

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Morning symptoms of rheumatoid arthritis (RA) are linked to circadian increase of night inflammation, supported by inadequate cortisol secretion in active disease. Therefore, exogenous glucocorticoid administration in RA is recommended by EULAR and ACR from the beginning of the diagnosis, since may partially act like a “replacement therapy”. In addition, the prevention/treatment of the night up-regulation of the immune/inflammatory reaction has been shown more effective when exogenous glucocorticoid administration is managed with a night-time-release formulation.Despite a considerably higher cost than conventional prednisone (immediate release), chronotherapy with night-time-release prednisone has been recognized a cost-effective option for RA patients not on glucocorticoids who are eligible for therapy with biologic disease-modifying antirheumatic drugs (DMARDs). Interestingly, since different cell populations involved in the inflammatory process are particularly activated during the night (i.e. monocytes, macrophages), other therapeutical approaches used in RA, such as conventional DMARDs and non-steroidal anti-inflammatory drugs (NSAIDs) should follow the same concepts of glucocorticoid chronotherapy. Therefore, bedtime methotrexate chronotherapy was found to better manage RA symptoms, and several available NSAIDs (i.e. indomethacin, aceclofenac, ketoprofen, flurbiprofen, lornoxicam) have been recently modified in their formulation, in order to obtain more focused night action.

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“…For example, a pH-responsive dual pulse multiparticulate dosage form containing ketoprofen was developed and tested in rheumatoid arthritis. Results showed that this formulation was able to relieve circadian symptoms during midnight and early morning [14]. Levi et al observed that the evening administration of indomethacin in a controlled release formulation was able to better control morning symptoms compared to the same formulation administered in other moment of the day [15].…”

Section: Introductionmentioning

confidence: 99%

NSAIDS: Design and Development of Innovative Oral Delivery Systems

Auriemma¹,

Cerciello²,

Aquino³

2017

Nonsteroidal Anti-Inflammatory Drugs

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Recently, different technologies have been used to transform active pharmaceutical ingredients (APIs) into new dosage forms. Engineered drug delivery systems may modify biopharmaceutical properties of the API achieving either immediate or delayed release according to specific therapeutic needs. Particularly, preprogrammed release of oral formulations delivering the drug at expected times may be useful in chronotherapy of early morning pathologies. The conventional approach when dealing with such diseases is to administer NSAIDs two to three times daily. This approach does not allow to fit drug release with symptoms onset resulting in inefficient therapy and poor patient compliance. NSAIDs may be very effective if administered at least 4-6 h before the pain reaches its peak in the early morning. The solution could be to design delayed drug delivery systems allowing one administration before going to sleep acting in the early morning. This chapter highlights new approaches in developing controlled delivery systems of NSAIDs potentially useful to treat both acute and chronic inflammation. The chapter illustrates the versatility of laminar jet break-up technology (prilling) to produce gel beads able to control rate and time of drug delivery. A special focus will be on particle-engineering strategies, i.e., prilling and prilling technique in tandem with microwave or supercritical fluid-assisted drying.

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pH-responsive dual pulse multiparticulate dosage form for treatment of rheumatoid arthritis

Abstract: The study concluded that the formulated multiparticulate dosage form of ketoprofen was able to relieve circadian symptoms of rheumatoid arthritis during midnight and early morning.

Cited by 16 publications

References 17 publications

Controlled Release of 5-Fluorouracil from Alginate Beads Encapsulated in 3D Printed pH-Responsive Solid Dosage Forms

Controlled Release of 5-Fluorouracil from Alginate Beads Encapsulated in 3D Printed pH-Responsive Solid Dosage Forms

Glucocorticoid management in rheumatoid arthritis: morning or night low dose?

NSAIDS: Design and Development of Innovative Oral Delivery Systems

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