A spotlight on thiolated natural polymers and their relevance in mucoadhesive drug delivery system

Naveen, N. Raghavendra; Gopinath, Chakka; Rao, D. Subba

doi:10.1016/j.fjps.2017.08.002

Cited by 17 publications

(13 citation statements)

References 50 publications

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“…Total tablet weight is adjusted concerning the animal body weight. After administration, radiographic images were captured at various time intervals to locate the location of the tablet and its disintegration (2 h and 10 h) (Naveen et al., 2018 ; Tang et al., 2018 ).…”

Section: Methodsmentioning

confidence: 99%

Compression-coated pulsatile chronomodulated therapeutic system: QbD assisted optimization

Aldawsari

Naveen²,

Alhakamy

et al. 2022

Drug Delivery

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Pulsatile drug delivery systems have drawn attention in contemporary research for designing chronotherapeutic systems. The current work aims to design pulsatile ketorolac tromethamine tablets using compression coating for delayed delivery with a lag time suitable for the treatment of morning stiffness in arthritis. Rapidly disintegrating core tablets of ketorolac tromethamine were formulated using super-disintegrants, and the optimized formulation was compression using PEO WSR coagulant and Eudragit RLPO for delaying the release. The central composite design and response surface methodology were employed to optimize the formulation and process parameters namely PEO WSR Coagulant (X 1 ), Eudragit RLPO (X 2 ), and Hardness (X 3 ). The dependent variables optimized were lag time and time required for 95% drug release. Analysis using response surface graphs and mathematical modeling of the results allowed identifying and quantifying the formulation variables active on the selected responses. A polynomial equation fitted to the data was used to predict the composition with optimum responses. Compression-coated pulsatile tablets’ optimized composition exhibited a lag time of 9 h and released 95% of the ketorolac tromethamine in 17.42 h. Validation of the mathematical model assured the reliability of QBD in formulation design. In vivo X-ray imaging and pharmacokinetic studies established a strong relationship between the coated polymers maintaining the desired lag time for delayed delivery of the active to coincide with the chronobiology for enhanced bioavailability at the right time when needed.

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Section: Methodsmentioning

confidence: 99%

Compression-coated pulsatile chronomodulated therapeutic system: QbD assisted optimization

Aldawsari

Naveen²,

Alhakamy

et al. 2022

Drug Delivery

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“…Solid dispersion is one of the technology that is explored broadly in the recent decades specially for the delivery of low soluble drugs [8] . Localization of conventional dosage forms can also results in enhancing the bioavailability as evident from several studies on coating [9] , mucoadhesion [10,11] , and floating approaches [12] . Fast dissolving tablets and matrix dosage forms are also established their application in enhancing the absorption [13,14] .…”

Section: Traditional Methodologies In Enhancing the Solubilitymentioning

confidence: 99%

Novel Approaches to Enhance Oral Bioavailability of Poorly Soluble Drugs

Gowthami

Krishna²,

Rao

2020

Int. J. Res. Pharm. Sci & Tech.

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Oral administration is considered as major, convenient route among all other routes of delivery, owing to several benefits. But, the poor solubility or enzymatic/metabolic activity are the major concerns in developing a successful formulation. About 40% of approved drugs which are in the current market and 90% of new drug molecules in the developmental pipeline are hydrophobic in nature. The challenge to formulate insoluble drugs has met with various approaches to overcome the problems related to solubility, application of nanotechnology is one amongst them. The present review deals with various nanocarriers and technologies that are proven to be effective in enhancing the bioavilability of poorly soluble drugs.

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“…In addition, their diverse molecular structures and the availability of functional chemical moieties in their molecular structures facilitate chemical modifications or functionalization like cross-linking, carboxymethylation, esterification, sulfation, phosphorylation, thiolation, grafting, etc., in order to introduce or improve derived functional properties [6][7][8][9]. Amongst these chemical modifications, a thiolation is a well-recognized approach to polysaccharide modification that imparts improvement of mucoadhesion of polysaccharides [10,11]. Thus, the above-mentioned chemical modifications can improve the applicability of different plant polysaccharides.…”

Section: Introductionmentioning

confidence: 99%

“…The term 'Biomucoadhesion' describes the adhesion of any system to the biological mucous membrane [10]. Mucoadhesive polymers are capable of prolonging contact as well as residence time when they are incorporated as mucoadhesive excipients in drug delivery systems [12].…”

Section: Introductionmentioning

confidence: 99%

“…In general, mucoadhesivity of the majority of polymers is associated with the formation of different kinds of non-covalent bonds like ionic interaction, hydrogen bonds, and Van der's Wall, which are weak bonds in nature [14,15]. Thus, these non-covalent bonds are not capable of providing high mucoadhesive contact and prolonging residence time [10,11]. As a result, the drug delivery system is unable to adhere to the mucous membrane of the target site over a prolonged period.…”

Section: Introductionmentioning

confidence: 99%

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Thiolation of Fenugreek Seed Polysaccharide; Utilization as a Novel Biomucoadhesive Agent in Drug Delivery

Bandyopadhyay

Nayak²

2023

Int J App Pharm

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Objective: The objectives of the present work were to carry out thiol-modification (i.e., thiolation) of fenugreek polysaccharide (FP) and to assess the synthesized thiolated product (TFP) as a mucoadhesive excipient in the designing of mucoadhesive formulations (metronidazole gels and metronidazole buccal discs). Methods: Extracted CG was thiol-modified via an esterification reaction by utilizing thioglycolic acid with an acidic milieu (using hydrochloric acid). Metronidazole mucoadhesive gels and buccal discs made of extracted FP and TFP (as mucoadhesive excipients) were prepared and evaluated to assess their biomucoadhesivity. Mucoadhesive gels containing 1%w/v metronidazole were prepared using both FP and TFP (1% w/v), separately. Mucoadhesive buccal discs containing metronidazole were prepared by the compression method, where FP and TFP (100 mg) were used as mucoadhesive excipients separately, along with 50 mg lactose and 25 mg PEG 4000. Results: The yield of TFP was 53.46% and the content of the thiol group in TFP was found to be 5.18 mmol of thiol group/g of FP. FTIR analysis results indicated the thiolation of FP in the synthesized TFP. Both types of formulations (mucoadhesive gels and buccal discs) made of TFP exhibited excellent improved ex vivo biomucoadhesion and a sustained pattern of metronidazole release over a prolonged period. Conclusion: The synthesized TFP can be used as improved mucoadhesive agent in the designing of biomucoadhesive systems for drug delivery.

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A spotlight on thiolated natural polymers and their relevance in mucoadhesive drug delivery system

Cited by 17 publications

References 50 publications

Compression-coated pulsatile chronomodulated therapeutic system: QbD assisted optimization

Compression-coated pulsatile chronomodulated therapeutic system: QbD assisted optimization

Novel Approaches to Enhance Oral Bioavailability of Poorly Soluble Drugs

Thiolation of Fenugreek Seed Polysaccharide; Utilization as a Novel Biomucoadhesive Agent in Drug Delivery

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