Lopinavir metered-dose transdermal spray through microporated skin: Permeation enhancement to achieve therapeutic needs

Patel, Amit B.; Kumar, Praveen; Thakkar, Hetal

doi:10.1016/j.jddst.2015.07.004

Cited by 14 publications

(5 citation statements)

References 24 publications

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“…The drug release from the MNs was through dissolution, as predicted by the Hixon–Crowell model (R 2 = 0.98). The n value (1.8) obtained by fitting the Korsemyer and Peppas model acknowledged super-case II transport drug release [ 32 , 33 ]. The super-case II transport corresponds to zero-order kinetics [ 34 ] (time-independent release), which is related to the relaxation behavior of the polymer happening upon water permeation into the MNs system as the rate-controlling step [ 35 ].…”

Section: Resultsmentioning

confidence: 99%

Hybrid Dissolving Microneedle-Mediated Delivery of Ibuprofen: Solubilization, Fabrication, and Characterization

et al. 2023

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Microneedles have recently emerged as a promising platform for delivering therapeutic agents by disrupting the skin, resulting in improved and high drug delivery via this route. Ibuprofen is widely used topically and orally for chronic pain conditions; to avoid untoward gastric effects, topical application is preferred over the oral route. This study aimed to enhance the solubility of the poorly water-soluble ibuprofen using Soluplus (SP) as a solubilizer and to fabricate dissolving microneedle patches of the drug. The fabricated patches were compared with marketed oral and topical formulations of ibuprofen. A 432-fold increase was observed in the solubility of the drug at 8% SP. The FTIR studies revealed that the drug and polymers were compatible. MNs were of uniform morphology and released the drug in a predictable manner. The in vivo analysis on healthy human volunteers revealed a Cmax of 28.7 µg/mL ± 0.5 with a Tmax of 24 h and a MRT of 19.5 h, which was significantly higher than that observed for commercially available topical formulations. The prepared ibuprofen microneedles have higher bioavailability and MRT at a lower dose (165 µg) as compared to tablet and cream doses (200 mg).

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Section: Resultsmentioning

confidence: 99%

Hybrid Dissolving Microneedle-Mediated Delivery of Ibuprofen: Solubilization, Fabrication, and Characterization

et al. 2023

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“…He found that tablets with hardness ranging between 19 and 21 kp, with no friability, capping, or lamination issue. D. Patel et al [44] formulated user-friendly metered-dose transdermal spray (MDTS) of lopinavir; he found that formulation containing 5 %w/v of Kollidon VA 64 had best sprayability and volatilisation property. Significantly increase in permeation enhancement and steady-state transdermal flux.…”

Section: Kollidon®va64 (Copovidone)mentioning

confidence: 99%

A brief review on Kollidon

Jagtap¹,

Tagad²,

Shendge

2019

J. Drug Delivery Ther.

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Polyvinylpyrrolidone includes soluble and insoluble grades; soluble grades are synthesised by the mechanism of polymerization, the free radical polymerization into water by using hydrogen peroxide as an initiator, the mechanism which terminates the polymerisation reaction makes it probable to produce soluble polyvinylpyrrolidone of about any molecular weight. Cross-linked polymer shows yield through popcorn polymerisation of an N-vinylpyrrolidone which gets insoluble polyvinylpyrrolidone. Kollidon is in the market as a brand name for polyvinylpyrrolidone, kollidon family now is a set of common excipients based on polyvinylpyrrolidone for use in pharmaceutical industry. They have a great variety of applications in an oral formulation; the functions of oral formulation encompass fast disintegration, sustain drug release, solubility, bioavailability enhancement, and stabilize the active ingredient. Kollidon containing a mixture of polyvinyl acetate plus povidone are generally used in the formation of sustained release formulation. Owing to their high molecular weight, are recognized as a suitable vehicle for producing sustained release drug delivery system. In this review paper, applications of different grades of kollidon are organized in the form of tables and reviewed critically. Current literature of patents on kollidon based formulations is also presented.

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“…In addition the system was found to be safe and stable as well as have potential to be used in clinical settings. 70…”

Section: Applications Of Evaporation Based Supersaturated Principlementioning

confidence: 99%

Transdermal Evaporation Drug Delivery System: Concept to Commercial Products

Parhi

Swain

2018

Adv Pharm Bull

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Since two decades or so transdermal route established itself as better alternative to traditional oral route. This is possible due to continuous innovations in transdermal drug delivery (TDD), which not only enables researchers from academia and industry to successfully develop and launch many new pharmaceuticals but also allow to include new classes of drugs that can be developed into transdermal formulations. These successes are achieved due to the use of novel techniques based on either physical or chemical approaches. However, both of these techniques suffer due to their own disadvantages. Comparatively, a simple method of supersaturation to enhance drug permeation across skin has created a new wave of interest. Even though the application supersaturated principle in topical and TDD has been used from 1960s, but proper control of drug release and formation of stable supersaturated states has been the core of intense research in the last decade. Out of various methods used to get supersaturated system, evaporation method is considered as most efficient and practically feasible for TDD. Therefore, in this review concept of supersaturation, selection of solvent system and the mechanism of inhibition of crystallization are discussed. Application of evaporation systems in the development of transdermal formulations such as solutions, semisolids and metered dose therapeutic systems (MDTS) and the commercial evaporative systems are also discussed in this review.

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Lopinavir metered-dose transdermal spray through microporated skin: Permeation enhancement to achieve therapeutic needs

Cited by 14 publications

References 24 publications

Hybrid Dissolving Microneedle-Mediated Delivery of Ibuprofen: Solubilization, Fabrication, and Characterization

Hybrid Dissolving Microneedle-Mediated Delivery of Ibuprofen: Solubilization, Fabrication, and Characterization

A brief review on Kollidon

Transdermal Evaporation Drug Delivery System: Concept to Commercial Products

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