Formulation Studies on Novel Self-Solidifying Self-Nanoemulsifying Drug Delivery Systems of Nebivolol Hydrochloride

Khutle, Nilesh; Vijaya, C

doi:10.2174/2211738502666141014212524

Cited by 3 publications

(2 citation statements)

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“…Primarily used for formulations containing Gelucire® 44/14 as a surfactant, this technique involves preparing a mixture of oil, surfactant, and co-surfactant and allowing it to solidify at room temperature or through freezing. Gelucire possesses both surfactant properties and the ability to solidify the mixture [38].…”

Section: Self-solidification By Surfactantmentioning

confidence: 99%

Revolutionizing Pharmaceuticals: A Deep Dive Into Self Nano Emulsifying Drug Delivery Systems

NIKAM,

JAIN,

SOLANKI

et al. 2024

Int J Curr Pharm Sci

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From nearly a decade’s time, there has been an increased inclination with respect to nanoemulsions owing to their augmented and ameliorated characteristics in comparison to conventional methods of drug delivery. Self-nano-emulsifying drug delivery systems (SNEDDS) have substantiated their effectiveness in enhancing the solubility and bioavailability of poorly soluble substances. These systems, often isotropic mixtures, consist of oils, surfactants, and cosurfactants/cosolvents. They possess the capability to create nanoemulsions or fine oil-in-water (o/w) emulsions with mild stirring and dilution by the water phase along the gastrointestinal tract. This system has proven its worth in enhancing the absorption of lipophilic agents constrained by dissolution rate. SNEDDS are extremely efficacious in improving the oral bioavailability of lipophilic products and is quite promising for managing drugs unapt for oral delivery. Additionally, it's noteworthy that SNEDDS can be formulated into various solid dosage forms suitable for both oral and parenteral administration. This overview incorporates the advancements of SNEDDS' the mechanism involved in its spontaneous formation, its subcategories, composition, approaches employed for formulation, characterization, merits and limitations, and future potential. The review also lays stress on the progress in solid self-emulsifying delivery mechanisms and dosage forms.

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Section: Self-solidification By Surfactantmentioning

confidence: 99%

Revolutionizing Pharmaceuticals: A Deep Dive Into Self Nano Emulsifying Drug Delivery Systems

NIKAM,

JAIN,

SOLANKI

et al. 2024

Int J Curr Pharm Sci

View full text Add to dashboard Cite

show abstract

“…Few studies have been carried out to overcome the current challenges associated with oral administration of nebivolol, and that can provide a controlled and effective delivery of nebivolol. Fast dissolving tablets, nanoparticles, self-nanoemulsifying delivery systems, transdermal systems etc were attempted to improve bioavailability of this drug but resulted with limited success [8,11]. Thus the therapeutic efficacy of nebivolol for the successful therapy remains elusive.…”

Section: Introductionmentioning

confidence: 99%

Development and Evaluation of Nebivolol Hydrochloride Nanocrystals Impregnated Buccal Film

Al‐Dhubiab¹

2019

FARMACIA

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Clinical efficacy of nebivolol is restricted primarily because of its low aqueous solubility and extensive hepatic metabolism. This study investigated the prospective of enhancing the systemic delivery of nebivolol HCl by formulating nanocrystals impregnated films for the buccal application. Nanocrystals of nebivolol HCl were prepared by acid-base neutralization method. Placebo films (N1-N3) were optimized by varying concentrations of chitosan. Further pure nebivolol HCl and its nanocrystals were incorporated to the films at two levels (2.5 mg/cm 2 and 5 mg/cm 2 ). The prepared films (N4-N7) were assessed for physicomechanical properties, swelling, drug release and permeation by standard protocols. Selected films were evaluated in vivo on rabbits. Physicomechanical properties displayed by the prepared films (N4-N7) were found to be adequate for the buccal application. Rapid swelling of films was noticed which would be beneficial and may contribute to immediate and effective bioadhesion with the buccal mucosa. The rate of drug dissolution was rapid and complete in 4 h from nanocrystals embedded films (N6 and N7) when compared to films loaded with pure drug. The permeation data indicates greater transport when drug concentration was higher (Film N7; 36.31 ± 6.54 µg/cm 2 /h; p < 0.0001). In vivo data signified rapid absorption (C max ~ 24 ng/mL) and higher AUC 0-α (~4 00 ng * h/mL) with ~ 2.5 folds improvement in the bioavailability. In conclusion, registered data suggests that the buccal application of nanocrystals embedded film improved the efficacy of nebivolol HCl, and necessitates further clinical studies. RezumatEficacitatea clinică a nebivololului este limitată în primul rând din cauza hidrosolubilității sale scăzute și a metabolismului hepatic intens. Acest studiu a investigat perspectiva creșterii biodisponibilității sistemice a clorhidratului de nebivolol prin formularea de filme impregnate cu nanocristale pentru aplicarea bucală. Nanocristalele de nebivolol HCI au fost preparate prin metoda de neutralizare acido-bazică. Filmele placebo (N1-N3) au fost optimizate prin utilizarea diferitelor concentrații de chitosan. Mai mult, nebivololul HCI pur și nanocristalele acestuia au fost încorporate în filme la două concentrații (2,5 mg/cm 2 și 5 mg/cm 2 ). Filmele preparate (N4-N7) au fost evaluate privind proprietățile lor fizico-mecanice, umflarea, eliberarea substanței active și permeabilitatea, folosind protocoalele standard. Filmul selectat a fost evaluat in vivo pe iepuri. Proprietățile fizico-mecanice afișate de filmele preparate (N4-N7) s-au dovedit a fi adecvate pentru aplicarea bucală. S-a observat umflarea rapidă a filmelor, care ar fi benefică și ar putea contribui la bioaderența imediată și eficientă pe mucoasa bucală. Procesul de dizolvare a fost rapid și complet, în 4 ore, pentru filmele încorporate în nanocristale (N6 și N7), în comparație cu filmele încărcate cu substanța pură. Datele de permeabilitate indică un transport mai eficient atunci când concentrația nebivolol HCl este mare (film N7; 36,...

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Self-microemulsifying Drug Delivery System for Problematic Molecules: An Update

Singh

Tiwary

Bedi

2019

NANOTEC

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Background: The poor bioavailability of a problematic molecule is predominantly due to its high lipophilicity, low solubility in gastric fluids and/or high fist pass metabolism. Self microemulsifying drug delivery system (SMEDDS), a lipidic type IV nano-formulation has been of interest in the field of pharmaceutical research due to its potential for tailoring the physicochemical properties of pharmaceutical molecules. Methods: This review provides insights on various recent innovations and reports from the past seven years (2012-2019) of self-emulsifying formulations for the delivery of various types of poorly soluble drugs, phytoconstituents and high molecular peptides and gives exhaustive details of the outcome of the endeavors in this field. Results: Various types of innovative formulations have been molded from SMEDDS like selfemulsifying powders, granules, tablets, pellets, eutectic and cationic formulations. Till date, many research reports and patents have been filed on self-emulsifying dosage forms and many formulations have gained US-FDA approvals which are summarized in the review article. Conclusion: This review content highlighted the increasing scope of SMEDDS in augmenting the physiochemical properties of an API, the variegated formulation types and the attributes of API that can be improved by SMEDD based formulations.

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Formulation Studies on Novel Self-Solidifying Self-Nanoemulsifying Drug Delivery Systems of Nebivolol Hydrochloride

Cited by 3 publications

References 0 publications

Revolutionizing Pharmaceuticals: A Deep Dive Into Self Nano Emulsifying Drug Delivery Systems

Revolutionizing Pharmaceuticals: A Deep Dive Into Self Nano Emulsifying Drug Delivery Systems

Development and Evaluation of Nebivolol Hydrochloride Nanocrystals Impregnated Buccal Film

Self-microemulsifying Drug Delivery System for Problematic Molecules: An Update

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