Formation of nanosuspensions in bottom-up approach: theories and optimization

Tehrani, Ali Ahmadi; Omranpoor, Mohammad Mahdi; Vatanara, Alireza; Seyedabadi, Mohammad; Ramezani, Vahid

doi:10.1007/s40199-018-00235-2

Cited by 73 publications

(35 citation statements)

References 164 publications

(346 reference statements)

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“…Lyophilization of the nanosuspensions shall be done to improve the physical and chemical stability and to overcome the incompatibilities between the various formulation components. Sterilization of the nanosuspensions can be done either by membrane filtration [79].…”

Section: Miscellaneous Methodsmentioning

confidence: 99%

“…Change in solvent causes high supersaturation conditions, which results in rapid nucleation and at the same time not allowing supersaturation near the nucleating crystals. Rapid nucleation and slow growth rate are the key decisive factors for successful thermodynamically stable crystal form according to classical Ostwald law of nucleation [79]. Generation of finely dispersed uniform sized drugs, simple and economical process and ease of scale-up are the main advantages of precipitation method.…”

Section: Manufacturing Techniques Precipitation Techniquesmentioning

confidence: 99%

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Emerging role of nanosuspensions in drug delivery systems

2020

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Rapid advancement in drug discovery process is leading to a number of potential new drug candidates having excellent drug efficacy but limited aqueous solubility. By virtue of the submicron particle size and distinct physicochemical properties, nanosuspension has the potential ability to tackle many formulation and drug delivery issues typically associated with poorly water and lipid soluble drugs. Conventional size reduction equipment such as media mill and high-pressure homogenizers and formulation approaches such as precipitation, emulsion-solvent evaporation, solvent diffusion and microemulsion techniques can be successfully implemented to prepare and scale-up nanosuspensions. Maintaining the stability in solution as well as in solid state, resuspendability without aggregation are the key factors to be considered for the successful production and scale-up of nanosuspensions. Due to the considerable enhancement of bioavailability, adaptability for surface modification and mucoadhesion for drug targeting have significantly expanded the scope of this novel formulation strategy. The application of nanosuspensions in different drug delivery systems such as oral, ocular, brain, topical, buccal, nasal and transdermal routes are currently undergoing extensive research. Oral drug delivery of nanosuspension with receptor mediated endocytosis has the promising ability to resolve most permeability limited absorption and hepatic first-pass metabolism related issues adversely affecting bioavailability. Advancement of enabling technologies such as nanosuspension can solve many formulation challenges currently faced among protein and peptide-based pharmaceuticals.

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Section: Miscellaneous Methodsmentioning

confidence: 99%

Section: Manufacturing Techniques Precipitation Techniquesmentioning

confidence: 99%

Emerging role of nanosuspensions in drug delivery systems

2020

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“…Examples for drugs prepared as nanosuspensions by these methods include griseofulvin, nabilone, atorvastatin. 16 The following methods are used to prepare nanosuspension,…”

Section: Methods Of Nanosuspensionmentioning

confidence: 99%

Nanosuspension as Promising and Potential Drug Delivery: A Review

Chinthaginjala¹,

Ahad²,

Reddy³

et al. 2022

Int J Life Sci Pharm Res

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In the last decade, nanosuspensions have gained considerable interest as a method for formulating poorly soluble drugs. Because of their cost-effectiveness and technological simplicity compared to liposomes and other colloidal drug carriers, nanoscale systems have recently received a lot of attention as a way of solving problems of solubility. Nanosuspensions are biphasic systems comprising of pure drug particles dispersed in an aqueous vehicle, stabilized by surface active agents. Fabrication of nanosuspension is simple and more advantageous than other approaches. Nanosuspension is a very finely single solid drug particle in an aqueous vessel, stabilized by surfactants for either oral or topical use or for parenteral and pulmonary administration, it can also be used for targeted drug delivery when incorporated in the ocular inserts and mucoadhesive hydrogels, with reduced particle size resulting in increased dissolution rate. This article covers the preparation of nanosuspension by bottom up technology, top down technology, melt emulsification, emulsification- solvent evaporation and supercritical fluid with their advantages and disadvantages, aspects of structure, classification and their drug delivery applications. Nanosuspension can be processed for the drugs which are of hydrophobic in nature quite easily employing stability enhancers, solvents that are of organic and additional ingredients including buffering agents, salts, PEG, osmotic agents and anti-freeze compounds.

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“…11,14,15 These techniques are advantageous as they lead to production of particles of homogeneous size ranges and require low energy and low temperature for thermolabile APIs and do not demand expensive instrumentation. 16 However, poor stability and requirement of high concentrations of emulsifiers remains a major concern for some of these techniques.…”

Section: ■ Introductionmentioning

confidence: 99%

“…Moreover, this technique further stands out from common nanosizing techniques employed in a pharmaceutical industrial setting such as hot-melt extrusion and wet milling, which are top-down in nature and energetically inefficient . In addition, the limited choice of excipients in the case of hot-melt extrusion and expensive instrumentation in the case of wet milling are some of the other drawbacks. , Bottom-up approaches such as spray-drying, freeze-drying, microfluidic crystallization, and formulation of APIs as nanoemulsions and polymer micelles have also been utilized. ,, These techniques are advantageous as they lead to production of particles of homogeneous size ranges and require low energy and low temperature for thermolabile APIs and do not demand expensive instrumentation . However, poor stability and requirement of high concentrations of emulsifiers remains a major concern for some of these techniques.…”

Section: Introductionmentioning

confidence: 99%

Drastic Modulation of Molecular Packing and Intrinsic Dissolution Rates by Meniscus-Guided Coating of Extremely Confined Pharmaceutical Thin Films

Kafle

Sanghavi

Khasbaatar

et al. 2021

ACS Appl. Mater. Interfaces

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Nanosizing has emerged as one of the most effective formulation strategies for enhancement of dissolution properties of active pharmaceutical ingredients (APIs). In addition to enhancing the specific area of the dissolving solids, nanosizing can also capture and stabilize the metastable form of the API, which can further enhance the solubility by drastic modulation of surface energies. Herein, we employ meniscus-guided coating to fabricate nanothin films of three APIs that show anticancer properties and are poorly soluble:10-HCPT, SN-38, and amonafide. By modulating the coating speed, we systematically deposited the APIs in films ranging from ∼200 nm thickness to extreme confinement of ∼10 nm (<10 molecular layers). In all three APIs, we observe a general order-to-disorder transition with semicrystalline (10-HCPT and amonafide) or amorphous (SN-38) form of API solids trapped in thin films when the thickness decreases below a critical value of ∼25–30 nm. The existence of a critical thickness highlights the importance of nanoconfinement in tuning molecular packing. In the case of 10-HCPT, we demonstrate that the disordered form of the API occurs largely due to lack of incorporation of water molecules in thinner films below the critical thickness, thereby disrupting the three-dimensional hydrogen-bonded network held by water molecules. We further developed a dissolution model that predicts variation of the intrinsic dissolution rate (IDR) with API film thickness, which also closely matched with experimental results. We achieved drastic improvement in the IDR of ∼240% in 10-HCPT by decreasing film thickness alone. Further leveraging the order-to-disorder transition led to 2570% modulation of the IDR for amonafide. Our work demonstrates, for the first time, opportunities to largely modulate API dissolution by precisely controlling the dimensionality of thin films.

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Formation of nanosuspensions in bottom-up approach: theories and optimization

Cited by 73 publications

References 164 publications

Emerging role of nanosuspensions in drug delivery systems

Emerging role of nanosuspensions in drug delivery systems

Nanosuspension as Promising and Potential Drug Delivery: A Review

Drastic Modulation of Molecular Packing and Intrinsic Dissolution Rates by Meniscus-Guided Coating of Extremely Confined Pharmaceutical Thin Films

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