Formulation and Release Characteristics of Zidovudine-Loaded Solidified Lipid Microparticles

Uronnachi, EM; Ogbonna, JDN; Kenechukwu, FC; Sa, Chime; Attama, AA; Okore, V. C.

doi:10.4314/tjpr.v13i2.5

Cited by 6 publications

(3 citation statements)

References 19 publications

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“…SLMs have the advantages of liposomes (possibility of controlled drug release and drug targeting), in addition to these advantages (use of non organic solvent, non-toxicity of the carrier system, chemical and physical storage stability for both the carrier and the drug, low cost of ingredients, not difficult in preparation and high scale-up potential) [7][8][9] . The most important limitation of SLMs is that drugs to be incorporated into SLMs must be lipophilic enough so as to ensure high-entrapment efficiency 10 and to overcome this problem, solid reversed micellar solution (SRMS)-based carriers have been investigated, and successfully employed to achieve controlled release of a hydrophilic drug, zidovudine 11 .…”

Section: Introductionmentioning

confidence: 99%

Formulation,in vitroandin vivoevaluation of halofantrine-loaded solid lipid microparticles

Ogbonna

Kenechukwu

Nwobi

et al. 2014

Pharmaceutical Development and Technology

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Context: Formulation, characterization, in vitro and in vivo evaluation of halofantrine-loaded solid lipid microparticles (SLMs). Objective: The objective of the study was to formulate and evaluate halofantrine-loaded SLMs. Materials and methods: Formulations of halofantrine-loaded SLMs were prepared by hot homogenization and thereafter lyophilized and characterized using particle size, pH stability, loading capacity (LC) and encapsulation efficiency (EE). In vitro release of halofantrine (Hf) from the optimized SLMs was performed in SIF and SGF. In vivo study using Peter's Four day suppressive protocol in mice and the mice thereafter subjected to histological studies in kidney and liver. Results: Results obtained indicated that EE of 76.32% and 61.43% were obtained for the SLMs containing 7% and 3% of Hf respectively. The SLMs loaded with 3% of Hf had the highest yield of 73.33%. Time-dependent pH stability analysis showed little variations in pH ranging from 3.49 ± 0.04 to 4.03 ± 0.05. Discussion: The SLMs showed pH-dependent release profile; in SIF (43.5% of the drug for each of H and H) compared with SGF (13 and 18% for H and H respectively) after 8 h. The optimized SLMs formulation and Halfan® produced a percentage reduction in parasitemia of 72.96% and 85.71% respectively. The histological studies revealed that the SLMs formulations have no harmful effects on the kidney and liver. Conclusion: SLMs formulations might be an alternative for patients with parasitemia as there were no harmful effects on vital organs of the mice.

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Section: Introductionmentioning

confidence: 99%

Formulation,in vitroandin vivoevaluation of halofantrine-loaded solid lipid microparticles

Ogbonna

Kenechukwu

Nwobi

et al. 2014

Pharmaceutical Development and Technology

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“…The yield of the drug determined the content of microcapsules formed at the end of the formulation as well as the quantity of polymer consumed during the preparation process [15].…”

Section: Discussionmentioning

confidence: 99%

Formulation and characterization of artemether-loaded sodium alginate microcapsules

Nnamani¹,

Echezona²,

Metu³

et al. 2020

Trop. J. Pharm Res

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Purpose: To increase the solubility of artemether (ART) in Transcutol® HP through microencapsulation in sodium alginate polymer to achieve sustained in vivo release.Method: Graded concentrations of ART (0.00, 0.25, 0.50, 0.75, and 1.00 g) microcapsules were produced using Tween® 80 by the cold homogenization method at 24 x 1000 rpm for 15 min. Characterization based on yield, encapsulation efficiency (EE), particle size, pH stability, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR) and in vivo release using Peter’s four-day suppressive protocol in Wistar mice infected with Plasmodium berghei, were determined.Results: The results obtained indicate that 0.5 g ART-loaded microcapsules (AMC) showed the highest yield of 96.85 %. The EE of 88.3 % corresponded to 0.75 g ART-loaded microcapsules. DSC results revealed that there was a significant reduction in enthalpy in all the formulations compared to the crystalline drug, but no strong bond interaction occurred except for the blank microcapsules. The AMC1.0 showed high dose-dependent plasmodial growth inhibition of 88.75 % while AMC0.25 had the least (68.13 %).Conclusion: The artemether microcapsules showed sustained release characteristics for oral delivery of artemether and therefore may reduce some of the adverse effects associated with high dose artemether therapy in conventional oral tablets. Keywords: Malaria, Artemether, Transcutol® HP, Sustained-release, RBC count, Antiplasmodial activity

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“…[18][19][20] Lipids can be an possible alternative to polymers in designing delivery devices for AZT as they would make a less biotoxic and efficient in provising spatial placement and temporal release. 21 The purpose of this study was to assess the utility of various lipids such as tripalmitin, trimyristin, and glyceryl monostearate in the formulation of solid lipid microparticles for zidovudine release stability, as well as the effect of soya lecithin on various properties of formulated zidovudine loaded solid lipid microparticles.…”

Section: Introductionmentioning

confidence: 99%

Utility of Different Lipids and Effect of Soya Lecithin on Sustained Delivery of Zidovudine via Biodegradable Solid Lipid Microparticles: Formulation and in-vitro Characterization

Sathyamoorthy¹,

Sundar²,

Rajendran³

et al. 2022

IJPER

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Background: Zidovudine (Azidothymidine, AZT) is widely used in the treatment of Acquired Immuno Deficiency Syndrome (AIDS) and related conditions, either alone or in combination with other antiviral agents to combat HIV. AZT is a Biopharmaceutical Classification System (BCS) class III drug and has various disadvantages. Thus, AZT is a potential candidate for delivery via lipid-based drug delivery system. Materials and Methods: In the present work, solid lipid microparticles (SLMs) of Zidovudine were developed for sustaining the drug release, to overcome or to reduce the hepatic metabolism and to ensure optimal bioavailability. A total of sixteen formulations of Zidovudine loaded solid lipid microparticles in two groups viz., one with tripalmitin and another with trimyristin were prepared by emulsion-solvent evaporation method. Results: The average particle size and entrapment efficiency of the prepared SLM varied between 5.48 µm-10.64 µm and 46.92 % and 58.39% respectively. The release of zidovudine from the SLM varied between 70.47% and 100% at the end of 24 hrs. 80% of the drug release which is required for obtaining the optimal therapeutic concentration was achieved by SLM 8. Conclusion: Formulation SLM 8 was considered best with maximum sustainability in the drug release along with maintaining therapeutic optimum. The formulation was found stable under stressed conditions.

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Formulation and Release Characteristics of Zidovudine-Loaded Solidified Lipid Microparticles

Abstract: Purpose: To formulate and determine the release profile of zidovudine (AZT)-loaded solidified lipid microparticles (SLMs

Cited by 6 publications

References 19 publications

Formulation,in vitroandin vivoevaluation of halofantrine-loaded solid lipid microparticles

Formulation,in vitroandin vivoevaluation of halofantrine-loaded solid lipid microparticles

Formulation and characterization of artemether-loaded sodium alginate microcapsules

Utility of Different Lipids and Effect of Soya Lecithin on Sustained Delivery of Zidovudine via Biodegradable Solid Lipid Microparticles: Formulation and in-vitro Characterization

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