Abstract:Acyclovir is an antiviral drug used for the treatment of herpes simplex virus infections, with an oral bioavailability of only 10–20% [limiting absorption in gastrointestinal tract to duodenum and jejunum] and half-life of about 3 h, and is soluble only at acidic pH (pKa 2.27). Mucoadhesive polymeric nanodrug delivery systems of acyclovir have been designed and optimized using 23 full factorial design. Poly (lactic-co-glycolic acid) (PLGA) (50:50) was used as the polymer along with polycarbophil (Noveon AA-1) … Show more
“…Generally, different release rates are attributed to different sizes of the NPs, but here the size of PLGA-PVP-NPs and PLGA-TPGS-NPs are almost comparable, hence size had no effect on the cumulative amount of ACY released in the two NPs. The initial rapid release of ACY could be as a result of the process by which PLGA undergoes biodegradation which exposes the drug closer to the surface (that could be free or loosely bound), in contact with the medium, to water that solubilizes the drug abruptly (Bhosale et al, 2011, Jain, 2000). Fig.…”
Delivering drugs via the ocular route has always been a challenge for poorly soluble drugs. The various anatomical and physiological barriers in the eye cavity hinder the residence of drugs within the corneal and precorneal regions. In this study, the nanosystem that could sufficiently deliver the poorly soluble Acyclovir topically via ocular route. Our nanosystem is composed of the biocompatible PLGA polymer stabilized with TPGS which possess a high emulsifying capacity and is also known as P-gp inhibitor. The optimized nanoparticles were prepared with 0.3% TPGS and had particle-size of 262.3 nm, zeta-potential of +15.14 mV. The physicochemical-characterization, ex vivo transcorneal permeation, ocular-irritation and Acyclovir ocular-availability, following topical ocular application of PLGA-NPs in rabbit eyes, were performed. The tested parameters and irritation by Draize’s test suggested the suitability and safety of PLGA-NPs for ocular use. An ultrahigh performance liquid chromatographic method was developed, validated, and applied to quantify Acyclovir in aqueous humor which was shown to be significantly higher (p < 0.05) using the developed nanoparticles as compared to Acyclovir-aqueous suspension following their single topical ocular administration. Noticeable 2.78-, 1.71- and 2.2-times increased values of AUC0–24h, t1/2 (h) and MRT0–24h were found, respectively, with the PLGA-TPGS-NPs as compared to ACY-AqS. These results demonstrate the superiority of delivering Acyclovir using a nanosystem compared to conventional methods.
“…Generally, different release rates are attributed to different sizes of the NPs, but here the size of PLGA-PVP-NPs and PLGA-TPGS-NPs are almost comparable, hence size had no effect on the cumulative amount of ACY released in the two NPs. The initial rapid release of ACY could be as a result of the process by which PLGA undergoes biodegradation which exposes the drug closer to the surface (that could be free or loosely bound), in contact with the medium, to water that solubilizes the drug abruptly (Bhosale et al, 2011, Jain, 2000). Fig.…”
Delivering drugs via the ocular route has always been a challenge for poorly soluble drugs. The various anatomical and physiological barriers in the eye cavity hinder the residence of drugs within the corneal and precorneal regions. In this study, the nanosystem that could sufficiently deliver the poorly soluble Acyclovir topically via ocular route. Our nanosystem is composed of the biocompatible PLGA polymer stabilized with TPGS which possess a high emulsifying capacity and is also known as P-gp inhibitor. The optimized nanoparticles were prepared with 0.3% TPGS and had particle-size of 262.3 nm, zeta-potential of +15.14 mV. The physicochemical-characterization, ex vivo transcorneal permeation, ocular-irritation and Acyclovir ocular-availability, following topical ocular application of PLGA-NPs in rabbit eyes, were performed. The tested parameters and irritation by Draize’s test suggested the suitability and safety of PLGA-NPs for ocular use. An ultrahigh performance liquid chromatographic method was developed, validated, and applied to quantify Acyclovir in aqueous humor which was shown to be significantly higher (p < 0.05) using the developed nanoparticles as compared to Acyclovir-aqueous suspension following their single topical ocular administration. Noticeable 2.78-, 1.71- and 2.2-times increased values of AUC0–24h, t1/2 (h) and MRT0–24h were found, respectively, with the PLGA-TPGS-NPs as compared to ACY-AqS. These results demonstrate the superiority of delivering Acyclovir using a nanosystem compared to conventional methods.
“…The mucoadhesion properties of NP studied using in vitro intestine model exhibited increased adhesiveness with raising levels of polycarbophil. [101] For the fabrication of single unit mucoadhesive tablets by direct compression method based on the 3 2 factorial design, the bioadhesive polymer namely carbopol 934P in addition with HPMC K100M was selected. These tablets have shown n-value varying between 0.5266 and 0.7110, to exhibit non-Fickian release with coupled diffusion and polymer relaxation, resulting in a controlled and complete drug release for 12 h. [102] Buccal bioadhesive tablets were formulated using spray dried amioca starch/carbopol 940P (5-45%) mixture at varying proportions, showed sustained release for 15 h. [103] Recently, the novel mucoadhesive formulation of ACV buccal tablet is commercialized with US FDA approval, for the treatment of recurring herpes labialis (cold sores).…”
T he guanine derivative antiviral drug acyclovir (ACV) is one of the oldest molecules laying successful market until date, being commercially available in various dosage forms for oral, topical and parenteral administrations. Clinical application of this drug is superior to new antiviral agents due to its potential values such as suppression of recurrence, safety profile, minimal drug interactions, and being inexpensive. ACV is slightly water-soluble, less permeable and poorly bioavailable, yet more potential antiviral molecule, the physicochemical modifications and novel dosage form approaches resulted with more than 100 research works within a decade. The survey of literature showed enormous reports on ACV formulation development, which includes modified tablets, particulate drug delivery, vesicular drug delivery, polymeric nanoparticles, bioadhesive systems, floating dosage forms, in situ gelling systems, transdermal delivery, implantable systems, emulsified dosage forms, polymeric films/patches, etc. As the drug could be administered via multiple routes for effective site targeted action at various doses, and attracted the attention of many researches, the review of the current approaches for the delivery of ACV could be more beneficial for the new scientists. This paper is a review of recent researches highlighting the development of newer techniques and novel dosage forms of ACV for better therapeutic efficacy, which were aimed at enhancing its solubility, permeability and bioavailability.Durai: Recent formulation designs of acyclovir How to cite this article: Durai RD. Drug delivery approaches of an antiviral drug: A comprehensive review. Asian J Pharm 2015;9:1-12.
“…PDI is a measure of homogeneity in dispersed systems and ranges from 0 to 1. Homogeneous dispersion has PDI value close to zero while PDI values greater than 0.5 suggest high heterogeneity [30].…”
Section: Particle Size Analyzer and Pdi Of Ind And Acv Loaded Nanoparmentioning
An eco-friendly nanoprecipitation technique was put forward to synthesize native starch nanoparticles loaded with insoluble drugs such as indomethacin (IND) and Acyclovir (ACV). Factors studied to find out the optimum conditions for preparation of different formulations of crosslinked starch nanoparticles (TPP-StNPs) loaded with insoluble drugs. The factors are 20 mg, 50 mg of drug concentration and 0.5, 1 g of sodium tripolyphosphate (STPP) while the concentration of starch and surfactant were kept constant. World-class facilities as particle size analyzer, poly dispersity index (PDI), zeta potential, TEM, XRD, FT-IR, UV-vis spectroscopy and DSc were used for evaluation of the resultant crosslinked starch nanoparticles loaded with drug. The sustained release of drugs were evaluated using entrapment efficiency and in vitro release. The data obtained confirmed that there is no chemical interaction between drug (IND, ACV) and crosslinked starch nanoparticles. The results indicate that the best formula for IND loaded starch nanoparticles was 0.5 g STPP and 20 mg IND while the best formula for ACV nanoparticles was at 0.5 g STPP and 50 mg ACV drug.
Indomethacin (IND), {2-{1-[(4-chlorophenyl) carbonyl]-5-Citation: El-Feky GS, El-Rafie MH, El-Sheikh MA, El-Naggar ME, Hebeish A (2015) Utilization of Crosslinked Starch Nanoparticles as a Carrier for Indomethacin and Acyclovir Drugs.
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