Biodegradable donepezil lipospheres for depot injection: optimization and in-vivo evaluation

Yehia, Soad A.; Elshafeey, Ahmed Hassen; Elsayed, Ibrahim

doi:10.1111/j.2042-7158.2012.01530.x

Cited by 18 publications

(4 citation statements)

References 44 publications

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“…This might be due to the pH dependent solubility of AMS (17). Increasing the pH of the external medium, to pH 12, and exceeding the pKa of AMS (9.37) kept the drug in its unionized form which is less soluble than the ionized drug, and reduced drug migration to the external phase (42).…”

Section: Effect Of the External Suspending Medium On Ee%mentioning

confidence: 99%

Enhanced Oral Absorption of Amisulpride Via a Nanostructured Lipid Carrier-Based Capsules: Development, Optimization Applying the Desirability Function Approach and In Vivo Pharmacokinetic Study

2019

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Amisulpride (AMS), a second generation antipsychotic, suffers from low oral bioavailability (48%). This might be due to its pH-dependent solubility or being a substrate of P-glycoprotein efflux pump. Nanostructured lipid carriers (NLCs) were proposed in this study to enhance the oral absorption of AMS. AMS-NLCs were prepared by solvent evaporation technique according to (2 1 .4 1 .3 1 ) factorial design, whereas the type of solid lipid (tripalmitin or Gelucire ® 43/1), lipid to drug ratio (7:1, 10:1, or 13:1) and type of external suspending medium (double distilled water, 0.5% TSP pH 12, 1% HPMC or 2.5% glycerin) were the independent variables. The average entrapment efficiency, particle size, polydispersity index, and zeta potential of the prepared formulations ranged from 29.01 to 69.06%, 184.9 to 708.75 nm, 0.21 to 0.59, and − 21 to − 33.55 mV, respectively. AMS-NLCs were optimized according to the desirability function to maximize the entrapment efficiency and minimize the particle size. Formulae G12, G10, and G7 with the highest desirability values of 0.915, 0.84, and 0.768, respectively, were chosen for further investigations. Novel AMS-NLCs capsules were prepared from the lyophilized formulations (TG7 and MG10) to enhance stability and increase patient compliance. The capsules were evaluated in terms of weight variation, content uniformity, and in vitro release pattern. The pharmacokinetics of AMS-NLCs capsules (formula TG7) were tested in rabbits compared to the commercial Amipride ® tablets. The relative bioavailability of AMS-NLCs capsules was found to be 252.78%. In conclusion, the NLC-based capsules show potential to improve the oral bioavailability of AMS.

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Section: Effect Of the External Suspending Medium On Ee%mentioning

confidence: 99%

Enhanced Oral Absorption of Amisulpride Via a Nanostructured Lipid Carrier-Based Capsules: Development, Optimization Applying the Desirability Function Approach and In Vivo Pharmacokinetic Study

2019

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“…Donepezil is used in the treatment of Alzheimer's patients, thus formulating it in a depot form is one of the great targets for these patients to decrease the frequency of administration and improve patient compliance. Accordingly, Intramuscular and subcutaneous liposphere injection helped in overcoming the burst release effect of the in-situ Donepezil formulation, and achieving depot effect and controlled release when compared to that of subcutaneous injection (Yehia et al, 2012a(Yehia et al, , 2012b. Based on the research work that was initiated by Hoffman et al in 2014, PNLs managed to improve the oral bioavailability of the drug by various mechanisms such as increasing GI drug solubilization, reducing the intra-enterocyte metabolism and reducing P-gp efflux activity.…”

Section: Parenteral Drug Deliverymentioning

confidence: 99%

Lipospheres and Pro-Nanolipospheres: Advancements in Drug Delivery Systems

Motawee

Khafagy²,

Gardouh³

et al. 2023

Records of Pharmaceutical and Biomedical Sciences

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The usefulness of nanotechnology nowadays in improving the performance of different active pharmaceutical ingredients (API) has generated a great deal of excitement worldwide. These nano-systems offer the advantage of higher bioavailability, lower toxicity, and the ability to deliver drugs with low half-life or low permeability. Lipid nano-based carriers have been extensively used for their ability to protect the API from degradation and their safety as these used lipids are generally regarded as safe. Lipospheres and Pro-nanolipospheres are among the promising systems for the delivery of water-insoluble drugs. They are composed of aqueous dispersible particles with a rigid hydrophobic lipid centre, coated by an outer protective phospholipid exterior. These lipospheres and Pro-nanolipospheres have the advantage of being easy to scale up, high dispersibility in aqueous media, and improved physical stability, making them the perfect candidate for the delivery of different APIs using different routes including oral, parenteral, intranasal and topical routes.

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“…[64] Oral particulate CsA liposphere dispersion was found to have improved bioavailability about 60%, while treating transplant rejection and autoimmune diseases. [65] Donepezil lipospheres were found to be efficacious in Alzheimer's treatment when it was administered as subcutaneous and intramuscular depot. [66] A formulation of buoyant lipospheres with lercanidipine, an antihypertensive agent was successfully proved as controlled delivery formulation.…”

Section: Applicationsmentioning

confidence: 99%

A perspective overview on lipospheres as lipid carrier systems

Dudala¹,

Yalavarthi²,

Vadlamudi³

et al. 2014

Int J Pharma Investig

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Both hydrophilic and lipophilic therapeutics can be delivered successfully into deep and peripheral tissues such as cerebrospinal fluid and central nervous system by encapsulating them with crystalline lipids as lipospheres. The advent of lipospheres was meant to deliver both therapeutic moieties with enhanced efficacy and added stability to reach out intended tissue areas. Although extensive information is available on physicochemical, analytical and biopharmaceutical aspects of lipospheres, there was no specific order pertaining to critical composition and rationale of component selection available for academic and pilot scale processing of lipospheres. With the interest of compiling key points in a typical formulation of lipid lipospheres, this article was intrigued to discuss melt method, co-solvent, microemulsion, super critical fluid, spray drying and spray congealing techniques that were employed to scale up lipospheres. The selection criteria for both the drugs and lipids in liposphere formulations were demonstrated here. The quality assessment with variables like loading capacity and entrapment efficiency was explained. A note on preliminary screening factors to determine the liposphere formation such as liposphere dimensions with morphological scenario was detailed in this article. This article also includes the stability and storage issues with reference to photolysis. The marked differential in enhancing solubility and permeability characteristics of Class II and IV drug candidates by liposphere delivery systems with an evident of in vivo outcomes were emphasized.

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Biodegradable donepezil lipospheres for depot injection: optimization and in-vivo evaluation

Abstract: Subcutaneous and intramuscular delivery of donepezil glyceryl tripalmitate lipospheres achieves depot release, allowing less frequent dosing.

Cited by 18 publications

References 44 publications

Enhanced Oral Absorption of Amisulpride Via a Nanostructured Lipid Carrier-Based Capsules: Development, Optimization Applying the Desirability Function Approach and In Vivo Pharmacokinetic Study

Enhanced Oral Absorption of Amisulpride Via a Nanostructured Lipid Carrier-Based Capsules: Development, Optimization Applying the Desirability Function Approach and In Vivo Pharmacokinetic Study

Lipospheres and Pro-Nanolipospheres: Advancements in Drug Delivery Systems

A perspective overview on lipospheres as lipid carrier systems

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