Improvement of physicochemical parameters of acyclovir using cocrystallization approach

Savjani, Jignasa; Pathak, Chirag

doi:10.1590/s1984-82502016000400017

Cited by 16 publications

(14 citation statements)

References 28 publications

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“…Group-specific molar volume contributions were tabulated using Fedor’s method and were taken from the literature . PLGA, curcumin, dexamethasone, nicotinamide, acyclovir, and solvent δ T , δ D , δ P , δ H , and V m were taken from the literature. − …”

Section: Methodsmentioning

confidence: 99%

Tyrosol Derived Poly(ester-arylate)s for Sustained Drug Delivery from Microparticles

Miles

Gwin

Zubris

et al. 2021

ACS Biomater. Sci. Eng.

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New biodegradable polymers are needed for use in drug delivery systems to overcome the high burst release, lack of sustained drug release, and acidic degradation products frequently observed in current formulations. Commercially available poly(lactide-co-glycolide) (PLGA) is often used for particle drug release formulations; however, it is often limited by its large burst release and acidic degradation products. Therefore, a biocompatible and biodegradable tyrosol-derived poly(ester-arylate) library has been used to prepare a microparticle drug delivery system which shows sustained delivery of hydrophobic drugs. Studies were performed using polymers with varying hydrophilicity and thermal properties and compared to PLGA. Various drug solubilizing cosolvents were used to load model drugs curcumin, dexamethasone, nicotinamide, and acyclovir. Hydrophobic drugs curcumin and dexamethasone were successfully loaded up to 50 weight percent (wt %), and a linear correlation between drug wt % loaded and the particle glass transition temperature (T g ) was observed. Both curcumin and dexamethasone were visible on the particle surface at 20 wt % loading and higher. By adjusting the polymer concentration during particle formation, release rates were able to be controlled. Release studies of dexamethasone loaded particles with a lower polymer concentration showed a biphasic release profile and complete release after 47 days. Particles prepared using a higher polymer concentration showed sustained release for up to 77 days. Comparably, PLGA showed a traditional triphasic release profile and complete release after 63 days. This novel tyrosol-derived poly(ester-arylate) library can be used to develop injectable, long-term release formulations capable of providing sustained drug delivery.

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Section: Methodsmentioning

confidence: 99%

Tyrosol Derived Poly(ester-arylate)s for Sustained Drug Delivery from Microparticles

Miles

Gwin

Zubris

et al. 2021

ACS Biomater. Sci. Eng.

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“…[14,15] Formulation-based approaches such as co-crystallization techniques were successfully employed for acyclovir to improve the solubility. [16] Co-solvency methods for Efavirenz were developed by Subramaneswari et al and reported to have better dissolution properties. [17] Hydrotropic methods, addition of solubilizing agents and ultra-rapid freeze technology were also reported to show improved bioavailability of the formulations.…”

Section: Enhancement Of Solubility and Dissolution Ratementioning

confidence: 99%

Untitled

2022

AJP

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Antiretroviral (ARV) therapy is a chemotherapeutic approach to treat viral infections such as AIDS. Remarkable therapeutic strategies improved the mortality rate in HIV patients. However, the neurocognitive disorders associated with HIV is not helmed properly due to the tight blood-brain barrier that restricts majority of ARVs to enter the brain parenchyma through the cerebral capillary endothelium. Conventional formulations are not adequate to reach these needs in the ARV therapy. Moreover, careful monitoring of pharmacokinetic parameters of the ARV drugs is important to achieve utmost therapeutic efficiency. However, the majority of the drugs are confronting this issue due to their poor aqueous solubility and inappropriate tissue permeability. Diversified nanotechnological and varied accustomed approaches were impended using novel polymers (both natural and synthetic) to ameliorate these pharmacokinetic constraints. Ample literature is available about the nanotechnological approaches allude to the development in the field for the enhancement of oral bioavailability, potency with less side effects. Nanotechnological cherishment also helps to control drug resistance and drug abuse. Making sub-micron level drug particles of poor water-soluble ARV drugs revamp the oral bioavailability by amplified surface area, improved interfacial tension at drug and solvent interface. The permeability issues are abolished by tailoring physical structure of the drug particle. Stability in the gastric environment, bypassing the early hepatic metabolism of ARV drugs also can be conquered with nanotechnological contrivances. Among all, nanocarrier, nano vesicular drug delivery system are well-crammed techniques. This review enumerates a detailed picture of bioavailability enhancement techniques for ARV drugs through nanotechnological advents.

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“…They found that the formation of co-crystals by the solvent evaporation method is better than the other methods used. 10…”

Section: Solvent Evaporation Techniquementioning

confidence: 99%

“…8 The co-crystals are held, by supramolecular heterosynthons that occur between the functional groups like carboxylic acid-aromatic nitrogen, carboxylic acidamide and alcohol-pyridine, with non-covalent forces, often including hydrogen bonding. 9,10 Other forces involved in co-crystallization are ionic and Van der Waals forces, lipophilic-lipophilic interactions and pi-pi interactions. 11 The co-crystals are different from that of salts due to less extent of proton transfer between drug and coformer.…”

Section: Introductionmentioning

confidence: 99%

Pharmaceutical Co-Crystallization: Regulatory Aspects, Design, Characterization, and Applications

et al. 2020

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Pharmaceutical co-crystals are novel class of pharmaceutical substances, which possess an apparent probability of advancement of polished physical properties offering stable and patentable solid forms. These multi-component crystalline forms influence pertinent physicochemical parameters like solubility, dissolution rate, chemical stability, physical stability, etc. which in turn result in the materials with superior properties to those of the free drug. Co-crystallization is a process by which the molecular interactions can be altered to optimize the drug properties. Co-crystals comprise a multicomponent system of active pharmaceutical ingredient (API) with a stoichiometric amount of a pharmaceutically acceptable coformer incorporated in the crystal lattice. By manufacturing pharmaceutical co-crystals, the physicochemical properties of a drug can be improved thus multicomponent crystalline materials have received renewed interest in the current scenario due to the easy administration in the pharmaceutical industry. There is an immense amount of literature available on co-crystals. However, there is a lack of an exhaustive review on a selection of coformers and regulations on co-crystals. The review has made an attempt to bridge this gap. The review also describes the methods used to prepare co-crystals with their characterization. Brief description on the pharmaceutical applications of co-crystals has also been incorporated here. Efforts are made to include reported works on co-crystals, which further help to understand the concept of co-crystals in depth.

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Improvement of physicochemical parameters of acyclovir using cocrystallization approach

Cited by 16 publications

References 28 publications

Tyrosol Derived Poly(ester-arylate)s for Sustained Drug Delivery from Microparticles

Tyrosol Derived Poly(ester-arylate)s for Sustained Drug Delivery from Microparticles

Untitled

Pharmaceutical Co-Crystallization: Regulatory Aspects, Design, Characterization, and Applications

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